Herbicidal sulfonamides

ABSTRACT

The invention relates to certain herbicidal sulfonamides, agriculturally suitable compositions thereof and a method for their use as a general or selective preemergent or postemergent herbicide or as a plant growth regulant.

RELATED APPLICATION

This application is a continuation of application Ser. No. 06/916,266, abandoned, filed Oct. 7, 1986, which is a continuation-in-part of copending application U.S. Ser. No. 801,120 filed Nov. 22, 1985, now abandoned which is a continuation-in-part of copending application U.S. Ser. No. 715,511 filed Mar. 27,1985 now abandoned which is a continuation-in-part of copending application U.S. Ser. No. 613,412 filed May 24, 1984, now abandoned.

BACKGROUND OF THE INVENTION

This invention relates to certain herbicidal sulfonamides, agriculturally suitable compositions thereof and a method for their use as a general or selective preemergent or postemergent herbicide or as a plant growth regulant.

New compounds effective for controlling the growth of undesired vegetation are in constant demand. In the most common situation, such compounds are sought to selectively control the growth of weeds in useful crops such as cotton, rice, corn, wheat and soybeans, to name a few. Unchecked weed growth in such crops can cause significant losses, reducing profit to the farmer and increasing costs to the consumer. In other situations, herbicides are desired which will control all plant growth. Examples of areas in which complete control of all vegetation is desired are areas around fuel storage tanks, ammunition depots and industrial storage areas. There are many products commercially available for these purposes, but the search continues for products which are more effective, less costly and environmentally safe.

The "sulfonylurea" herbicides are an extremely potent class of herbicides discovered within the last few years which generally consist of a sulfonylurea bridge, --SO₂ NHCONH--, linking two aromatic or heteroaromatic rings.

U.S. Pat. No. 4,394,506 discloses herbicidal ortho-alkoxycarbonylbenzenesulfonamides such as ##STR1## wherein R₂ is H, F, Cl, Br, C₁ -C₃ alkyl, NO₂, SO₂ CH₃, OCH₃, SCH₃, CF₃, N(CH₃)₂, NH₂ or CN;

X is H, Cl, CH₃, OCH₃, OCH₂ CH₃ or OCH₂ CH₂ OCH₃ ; and

Y is H, halogen, C₁ -C₄ alkyl, C₁ -C₄ substituted alkyl, C₁ -C₄ alkoxy, etc.

South African patent application No. 81/4874 discloses herbicidal sulfonamides of formula ##STR2## wherein A is a C₁ -C₆ alkyl radical which is substituted by halogen or various other organic substituents or a C₂ -C₆ alkenyl radical which is substituted or unsubstituted;

X is O, S, SO or SO₂ ;

R₁ is H, halogen, C₁ -C₅ alkyl, C₂ -C₅ alkenyl or YR₅ ;

R₂ is H, halogen, C₁ -C₅ alkyl, C₂ -C₅ alkenyl, C₁ -C₄ haloalkyl, CO₂ R₆, YR₅, NO₂ or CONR₇ R₈ ; and

R₃ and R₄, each independently of the other, are hydrogen, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, C₁ -C₄ alkylthio, C₁ -C₄ haloalkyl, halogen or alkoxyalkyl of at most 4 carbon atoms.

South African patent application No. 82/5042 discloses herbicidal sulfonamides of formula ##STR3## wherein A is C₃ -C₆ alkynyl;

X is O, S, SO or SO₂ ;

R₁ is H, halogen, C₁ -C₅ alkyl, C₂ -C₅ alkenyl or YR₅ ;

R₂ is H, halogen, C₁ -C₅ alkyl, C₂ -C₅ alkenyl, C₁ -C₄ haloalkyl, CO₂ R₆, YR₅, NO₂ or CONR₇ R₈ ; and

R₃ and R₄, independently of one another, are hydrogen, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, C₁ -C₄ alkylthio, C₁ -C₄ haloalkyl, C₁ -C₄ haloalkoxy, halogen or alkoxyalkyl of at most 4 carbon atoms.

South African patent application No. 82/5671 discloses herbicidal sulfonamides of formulas ##STR4## wherein A is a C₁ -C₆ alkyl radical or a C₂ -C₆ alkenyl radical which is substituted by halogen or various other organic substituents;

X is O, S, SO or SO₂ ;

R₁ is H, halogen, C₁ -C₅ alkyl, C₂ -C₅ alkenyl or YR₅ ;

R₂ is H, halogen, C₁ -C₅ alkyl, C₂ -C₅ alkenyl, C₁ -C₄ haloalkyl, CO₂ R₆, YR₅, NO₂ or CONR₇ R₈ ;

R₃ is hydrogen, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, C₁ -C₄ alkylthio, C₁ -C₄ haloalkyl, C₁ -C₄ haloalkoxy, halogen or alkoxyalkyl of at most 4 carbon atoms; and

R₄ is C₁ -C₄ haloalkoxy or C₁ -C₄ haloalkylthio.

South African patent application No. 83/0127 discloses herbicidal sulfonamides of formula ##STR5## wherein R₁ is hydrogen, halogen, cyano, nitro, C₁ -C₄ haloalkyl, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, COR₆, NR₇ R₈, S(O)_(m) --C₁ -C₄ alkyl or SO₂ R₉ ;

R₂ is H, F, Cl, Br, NO₂, CF₃, NR₂₀ R₂₁, C₁ -C₂ alkyl, C₁ -C₂ alkoxy or S(O)_(m) --C₁ -C₄ alkyl;

R₃ is H, F, Cl, Br, NH₂, NO₂ or OCH₃ ;

R₆ is hydrogen, C₁ -C₄ alkyl, C₃ -C₅ alkenyloxy, C₃ -C₅ alkynyloxy, C₁ -C₄ haloalkyl, C₁ -C₅ alkylthio, phenoxy, benzyloxy, NR₁₀ R₁₁ or C₁ -C₅ alkoxy which is unsubstituted or substituted by 1-3 halogen atoms or C₁ -C₃ alkoxy;

R₁₈ is hydrogen, C₁ -C₃ alkyl or C₁ -C₃ alkoxy;

m is 0, 1 or 2; and

Y is C₁ -C₃ alkyl, C₁ -C₃ haloalkyl, C₁ -C₃ alkoxy, C₁ -C₃ haloalkoxy, C₂ -C₃ alkoxyalkyl, C₁ -C₃ alkylthio, halogen or NR₁₆ R₁₇.

South African patent application No. 84/2245 discloses herbicidal sulfonamides of formula ##STR6## wherein A is C₁ -C₆ haloalkyl;

R₁ is hydrogen, halogen, nitro, cyano, C₁ -C₄ alkyl, C₁ -C₄ haloalkyl, C₁ -C₄ alkoxy, C₁ -C₄ alkylthio, C₁ -C₄ alkylsulfinyl, C₁ -C₄ alkylsulfonyl, COR₆, NR₇ R₈, CONR₉ R₁₀ or SO₂ NR₁₁ R₁₂ ;

R₂ is hydrogen, halogen, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, C₁ -C₄ alkylthio, C₁ -C₄ alkylsulfinyl or C₁ -C₄ alkylsulfonyl; and

R₃ and R₄, independently of one another, are each hydrogen, halogen, C₁ -C₄ alkyl, C₁ -C₄ haloalkyl, C₂ -C₄ haloalkoxy, C₁ -C₄ alkylthio, C₁ -C₄ haloalkylthio, C₂ -C₄ alkoxyalkyl, C₁ -C₄ alkoxy or NR₁₂ R₁₃.

South African patent application No. 84/2722 discloses herbicidal benzenesulfonamides of formula ##STR7## wherein A is a radical of the formula CR₆ R₇ XR₈, CR₉ R₁₀ R₁₁ or CHR₇ SCQR₂₁ ;

R₁ is hydrogen, halogen, nitro, cyano, C₁ -C₄ alkyl, C₁ -C₄ haloalkyl, YR₁₄, CONR₁₂ R₁₃, NR₁₂ R₁₃, SONR₁₅ R₁₆, OSO₂ R₁₇ or COR₁₈ ;

R₂ is hydrogen, halogen, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, C₁ -C₄ alkylthio, C₁ -C₄ alkylsulfinyl or C₁ -C₄ alkylsulfonyl;

R₃ and R₄, independently of one another, are each hydrogen, halogen, C₁ -C₄ alkyl, C₁ -C₄ haloalkyl, C₁ -C₄ alkoxy, C₁ -C₄ haloalkoxy, C₁ -C₄ alkylthio, C₁ -C₄ haloalkylthio, C₂ -C₅ alkoxyalkyl or NR₁₉ R₂₀ ;

R₉ is hydrogen, halogen, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, C₁ -C₄ alkylthio, C₁ -C₄ alkylsulfinyl or C₁ -C₄ alkylsulfonyl;

R₁₀ is hydrogen, halogen or methyl;

R₁₁ is a radical COR₂₄ or a C₁ -C₄ alkyl group that is mono- or polysubstituted by substituents selected from the group: cyano, nitro, hydroxyl, C₁ -C₄ alkoxy, C₁ -C₄ alkylthio, etc.

R₁₈ is H, C₁ -C₄ alkoxy and various other organic radicals.

South African patent application No. 83/0041 discloses herbicidal benzenesulfonamides of formula ##STR8## wherein R₁ is H, halogen, NO₂, C₁ -C₄ haloalkyl, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, C₂ -C₅ alkenyl or C₁ -C₄ alkoxycarbonyl;

R₂ is C₁ -C₃ alkyl or C₁ -C₃ alkoxy, each unsubstituted or substituted by 1 to 3 halogen atoms;

R₃ is halogen, H, NR₄ R₅, C₁ -C₃ alkyl, unsubstituted or substituted by 1 to 3 halogen atoms ro C₁ -C₄ alkoxy, or is C₁ -C₃ alkoxy, unsubstituted or substituted by methoxy, ethoxy, or 1 or 3 halogen atoms;

A is C₁ -C₄ alkylene or C₂ -C₄ alkenylene, each unsubstituted or substituted by C₁ -C₄ alkyl;

m is 0 or 1;

E is N or CH;

X is oxygen, sulfur, SO or SO₂ ; and

Q is, in part, OH, CN, NR₆ R₇, SO₂ R₈, cycloalkyl or COCH₁ -C₆ alkyl.

South African patent application No. 83/3779 discloses herbicidal benzenesulfonamides of formula ##STR9## wherein A is C.tbd.CR;

m is 1 or 2;

E is CH or N;

Z is oxygen or sulfur,

R is, in part, H, C₁ -C₉ alkyl or C₁ -C₉ haloalkyl;

R₁ is H, halogen, C₁ -C₅ alkyl, C₂ -C₅ alkenyl or YR₅ ;

R₂ is H, halogen, C₁ -C₅ alkyl, C₂ -C₅ alkenyl, C₁ -C₄ haloalkyl, YR₅, CO₂ R₆, NO₂ or CONR₇ R₈ ;

R₃ and R₄, each independently of the other, are H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, C₁ -C₄ alkylthio, C₁ -C₄ haloalkyl, C₁ -C₄ haloalkoxy, C₁ -C₄ haloalkylthio, halogen, C₂ -C₅ alkoxyalkyl, NR₉ R₁₀ or OCH₂ CH₂ NR₉ R₁₀.

There is however a continuing need to find herbicides that are more effective and more selective toward agricultural products.

SUMMARY OF THE INVENTION

This invention relates to novel compounds of Formula I, agriculturally suitable compositions containing them and their method-of-use as general or selective preemergent or postemergent herbicides or as plant growth regulants. ##STR10## wherein R is H or CH₃ ;

R₁ is C₁ -C₃ alkyl, C₃ -C₄ alkoxylalkyl, C₂ -C₄ haloalkyl, C₃ -C₄ alkenyl or C₃ -C₄ alkynyl;

R₂ is C₁ -C₃ alkyl, cyclopropyl, C₁ -C₃ alkoxy, C₁ -C₃ alkylthio, C₁ -C₃ alkylsulfinyl, C₁ -C₃ alkylsulfonyl, allyloxy, allylthio, allysulfinyl, allylsulfonyl, propargyloxy, propargylthio, propargylsulfinyl, propargylsulfonyl, C₁ -C₃ haloalkoxy, C₁ -C₃ alkyl substituted with 1-3 atoms of F or Cl, C₁ -C₂ alkyl substituted with C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ ∝C₂ alkylthio, C₁ -C₂ haloalkylthio, C₁ -C₂ alkylsulfinyl, C₁ -C₂ haloalkylsufinyl, C₁ -C₂ alkylsulfonyl, C₁ -C₂ haloalkylsulfonyl, OH or OC(O)C₁ -C₂ alkyl, C₁ -C₂ alkoxy substituted with C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio, C₁ -C₂ alkylsulfinyl, C₁ -C₂ haloalkylsulfinyl, C₁ -C₂ alkylsulfonyl, C₁ -C₂ haloalkylsulfonyl or CN, OCH₂ CH₂ NH₂, OCH₂ CH₂ NHCH₃, OCH₂ CH₂ N(CH₃)₂, C₁ -C₂ alkylthio substituted by C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio or CN, C₁ -C₃ haloalkylthio, C₁ -C₃ haloalkylsulfinyl, C₁ -C₃ haloalkylsulfonyl, C₂ -C₃ alkenyl, C.tbd.CH, NR_(b) R_(c) or OC(O)C₁ -C₂ alkyl;

R_(b) is H or C₁ -C₂ alkyl;

R_(c) is C₁ -C₂ alkyl or C₁ -C₂ haloalkyl;

Y is CH₃, OCH₃ or OCF₂ H; and

their agriculturally suitable salts.

In the above definitions, the term "alkyl", used either alone or in compound words such as "alkylthio" or "haloalkyl", denotes straight chain or branched alkyl, e.g., methyl, ethyl, n-propyl or isopropyl.

Alkoxy denotes methoxy, ethoxy, n-propoxy or isopropoxy.

Alkenyl denotes vinyl, 1-propenyl, 2-propenyl or 3-propenyl.

The term "halogen", either alone or in compound words such as "haloalkyl", denotes fluorine, chlorine, bromine or iodine. Further, when used in compound words such as "haloalkyl" said alkyl may be partially or fully substituted with halogen atoms, which may be the same or different. Examples of haloalkyl include CH₂ CH₂ F, CF₂ CF₃ and CH₂ CHFCl.

The total number of carbon atoms in a substituent group is indicated by the C_(i) -C_(j) prefix where i and j are numbers from 1 to 3. For example, C₁ -C₃ alkylsulfonyl would designate methylsulfonyl through propylsulfonyl.

Preferred for their higher herbicidal activity, greater plant growth regulant activity and/or more favorable ease of synthesis are:

1. Compounds of Formula I wherein R₂ is C₁ -C₃ alkyl, cyclopropyl, C₁ -C₃ alkoxy, C₁ -C₃ alkylthio, C₁ -C₃ alkylsulfinyl, C₁ -C₃ alkylsulfonyl, allyloxy, allylthio, allylsulfinyl, allylsulfonyl, propargyloxy, propargylthio, propargylsulfinyl, propargylsulfonyl, OCF₂ H, OCH₂ CH₂ F, OCH₂ CHF₂, OCH₂ CF₃, OCH₂ CH₂ Cl or C₁ -C₃ alkyl substituted with 1-3 atoms of F or Cl, C₁ -C₂ alkyl substituted with OCH₃ or SCH₃.

2. Compounds of Preferred (1) wherein R₂ is C₁ -C₂ alkyl, C₁ -C₂ alkoxy, C₁ -C₃ alkylthio, C₁ -C₃ alkylsulfinyl, C₁ -C₃ alkylsulfonyl, CF₃, propargyloxy, propargylthio, propargylsulfinyl, propargylsulfonyl, OCF₂ H, OCH₂ CH₂ F, OCH₂ CHF₂, OCH₂ CF₃, OCH₂ CH₂ Cl, CH₂ CH₂ OCH₃ or CH₂ CH₂ SCH₃.

3. Compounds of Preferred (2) wherein

R is H;

R₁ is C₁ -C₂ alkyl;

R₂ is C₁ -C₂ alkyl, C₁ -C₂ alkoxy, C₁ -C₂ alkylthio, CF₃ or OCF₂ H; and

Y is CH₃ or OCH₃.

4. Compounds of Preferred (3) wherein R₂ is CH₃, OCH₃, OCH₂ CH₃ or CF₃.

5. Compounds of Formula I wherein R₂ is n-propyl, isopropyl, cyclopropyl, n-propoxy, isopropoxy, allyloxy, allylthio, allylsulfinyl, allylsulfonyl, C₂ -C₃ alkenyl, OC(O)CH₃, OC(O)CH₂ CH₃, CH₂ F, CHF₂, C₂ -C₃ alkyl substituted with 1-3 atoms of F, C₁ -C₃ alkyl substituted with 1-3 atoms of Cl, CH₂ OH, CH(CH₃)OH, CH₂ OCH₃, CH₂ OCH₂ CH₃, CH₂ (CH₃)OCH₃, CH₂ (CH₃)OCH₂ CH₃, CH₂ SCH₃, CH₂ SCH₂ CH₃, CH₂ (CH₃)SCH₃, CH₂ (CH₃)SCH₂ CH₃, CH₂ OC(O)C₁ -C₂ alkyl, CH(CH₃)OC(O)C₁ -C₂ alkyl, CH₂ OC₁ -C₂ haloalkyl of at least 3 halogens, CH₂ SC₁ -C₂ haloalkyl of at least 3 halogens, CH₂ S(O)C₁ -C₂ haloalkyl of at least 3 halogens, CH₂ SO₂ C₁ -C₂ haloalkyl of at least 3 halogens, CH.sub.(CH₃)OC₁ -C₂ haloalkyl of at least 3 halogens, CH(CH₃)SC₁ -C₂ haloalkyl of at least 3 halogens, CH(CH₃)S(O)C₁ -C₂ haloalkyl of at least 3 halogens, CH(CH₃)SO₂ C₁ -C₂ haloalkyl of at least 3 halogens, CH₂ CH₂ S(O)C₁ -C₂ haloalkyl or CH₂ CH₂ SO₂ C₁ -C₂ haloalkyl.

6. Compounds of Preferred (5) wherein R₂ is propyl, isopropyl, cyclopropyl, propoxy, isopropoxy, allyloxy, allylthio, allylsulfinyl, allylsulfonyl, CH₂ OCH₃, CH(CH₃)OCH₃, CH₂ SCH₃, CH(CH₃)SCH₃, CH₂ F, CHF₂, C₂ -C₃ alkyl substituted with 1-3 atoms of F or C₁ -C₃ alkyl substituted with 1-3 atoms of Cl.

7. Compounds of Formula I wherein R₂ is C₁ -C₃ alkyl, OCH₃, SCH₃, SO₂ CH₃, CF₃ or NR_(b) R_(c).

8. Compounds of Formula I wherein R₂ is C₁ -C₂ alkoxy substituted with CN, OCH₂ CH₂ NH₂, OCH₂ CH₂ N(CH₃) or C₁ -C₂ alkylthio substituted by CN.

9. Compounds of Preferred (8) wherein R₂ is OCH₂ CH₂ CN, OCH₂ CH₂ NH₂, OCH₂ CH₂ N(CH₃) or SCH₂ CH₂ CN.

10. Compounds of Formula I wherein R₂ is CH₂ CH₂ OC₁ -C₂ alkyl, CH₂ CH₂ SC₁ -C₂ alkyl, CH₂ CH₂ S(O)C₁ -C₂ alkyl, CH₂ CH₂ SO₂ C₁ -C₂ alkyl, CH₂ CH₂ OC₁ -C₂ haloalkyl, CH₂ CH₂ SC₁ -C₂ haloalkyl, CH₂ OC₁ -C₂ haloalkyl of 1 or 2 halogens, CH₂ SC₁ -C₂ haloalkyl of 1 or 2 halogens, CH₂ S(O)C₁ -C₂ haloalkyl of 1 or 2 halogens, CH₂ SO₂ C₁ -C₂ haloalkyl of 1 or 2 halogens, CH(CH₃)OC₁ -C₂ haloalkyl of 1 or 2 halogens, CH(CH₃)SC₁ -C₂ haloalkyl of 1 or 2 halogens, CH(CH₃)S(O)C₁ -C.sub. 2 haloalkyl of 1 or 2 halogens, or CH(CH₃)SO₂ C₁ -C₂ haloalkyl of 1 or 2 halogens.

11. Compounds of Formula I wherein R₂ is propargyloxy, propargylthio, propargylsulfinyl or propargylsulfonyl.

12. Compounds of Formula I wherein R₂ is allyloxy, allylthio, allylsulfinyl, allylsulfonyl, C₁ -C₃ haloalkoxy, C₁ -C₂ alkoxy substituted with C₁ -C₂ alkoxy, C₁ -C₂ haloalkyl, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio, C₁ -C₂ alkylsulfinyl, C₁ -C₂ haloalkylsulfinyl, C₁ -C₂ alkylsulfonyl or C₁ -C₂ haloalkylsulfonyl, C₁ -C₃ haloalkylthio, C₁ -C₃ haloalkylsulfinyl or C₁ -C₃ haloalkylsulfonyl.

13. Compounds of Preferred (12) wherein R₂ is allyloxy, allylthio, allylsulfinyl, allylsulfonyl, OCF₂ H, OCH₂ CF₃, OCH₂ CH₂ OCH₃, OCH₂ CH₂ OCH₂ CH₃, OCH₂ CH₂ OCH₂ CF₃, OCH₂ CH₂ OCF₂ H, OCH₂ CH₂ SCH₃, OCH₂ CH₂ SCH₂ CF₃, OCH₂ CH₂ S(O)CH₃, OCH₂ CH₂ S(O)CH₂ CF₃, OCH₂ CH₂ SO₂ CH₃, OCH₂ CH₂ SO₂ CH₂ CF₃, SCF₂ H, SCH₂ CF₃, S(O)CH₂ CF₃ or SO₂ CH₂ CF₃.

14. Compounds of Formula I wherein R₂ is C₁ -C₃ haloalkoxy, C₁ -C₂ alkoxy substituted with C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio, C₁ -C₂ alkylsulfinyl, C₁ -C₂ haloalkylsulfinyl, C₁ -C₂ alkylsulfonyl or C₁ -C₂ haloalkylsulfonyl, C₁ -C₂ alkylthio substituted by C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio or C₁ -C₂ haloalkylthio, C₁ -C₃ haloalkylthio, C₁ -C₃ haloalkylsulfinyl or C₁ -C₃ haloalkylsulfonyl.

15. Compounds of Preferred (14) wherein R₂ is OCF₂ H, OCH₂ CF₃, OCH₂ CH₂ OCH₃, OCH₂ CH₂ OCH₂ CH₃, OCH₂ CH₂ OCH₂ CF₃, OCH₂ CH₂ OCF₂ H, OCH₂ CH₂ SCH₃, OCH₂ CH₂ SCH₂ CF₃, OCH₂ CH₂ S(O)CH₃, OCH₂ CH₂ S(O)CH₂ CF₃, OCH₂ CH₂ SO₂ CH₃, OCH₂ CH₂ SO₂ CH₂ CF₃, SCH₂ CH₂ OCH₃, SCH₂ CH₂ OCH₂ CH₃, SCH₂ CH₂ OCH₂ CF₃, SCH₂ CH₂ SCH₃, SCH₂ CH₂ SCH₂ CF₃, SCF₂ H, SCH₂ CF₃, S(O)CH₂ CF₃ or SO₂ CH₂ CF₃.

16. Compounds of Formula I wherein R₂ is C₁ -C₃ alkyl substituted with 1-3 atoms of F of Cl.

17. Compounds of Preferred (16) wherein R₂ is CF₃, CF₂ H, CFH₂, CCl₂ H or CH₂ Cl.

18. Compounds of Formula I wherein R₂ is C₁ -C₂ alkyl, C₁ -C₂ alkoxy, C₁ -C₃ alkylthio, C₁ -C₃ alkylsulfinyl, C₁ -C₃ alkylsulfonyl, CF₃ or NR_(b) R_(c).

19. Compounds of Preferred (18) wherein R₂ is CH₃, CH₂ CH₃, OCH₃, OCH₂ CH₃, SCH₃, SCH₂ CH₃, SCH(CH₃)₂, S(O)CH₃, S(O)CH₂ CH₃, S(O)CH(CH₃)₂, SO₂ CH₃, SO₂ CH₂ CH₃, SO₂ CH(CH₃)₂, CF₃, NHCH₃ or N(CH₃)₂.

20. Compounds of Formula I wherein R₂ is C.tbd.CH.

Specifically preferred for its highest herbicidal activity, greatest plant growth regulant activity and/or most favorable ease of synthesis is: 2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic acid, methyl ester, m.p. 195°-196° C.

The invention also relates to agriculturally suitable compositions for controlling the growth of undesired vegetation comprising an effective amount of a compound recited above and at least one of the following: surfactant, solid or liquid diluent.

The invention also relates to a method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of the invention.

DETAILED DESCRIPTION OF THE INVENTION Synthesis

The compounds of Formula I can be prepared by one or more of the following methods described in Equations 1 to 3 and 14.

As shown in Equation 1, compounds of Formula I can be prepared by reacting an appropriately substituted sulfonyl isocyanate of Formula (1) with an appropriate amino or methylamino heterocycle of Formula (2). Y, R, R₁, and R₂ are as previously defined. ##STR11##

The reaction is best carried out in inert aprotic organic solvents such as dichloromethane, 1,2-dichloroethane, tetrahydrofuran, or acetonitrile, at a temperature between 20° and 85° C. The order of addition is not critical; however, it is often convenient to add the sulfonyl isocyanate or a solution of it in the reaction solvent to a stirred suspension of the amine.

In some cases, the desired product is insoluble in the reaction solvent at ambient temperature and crystallizes from it in pure form. Products soluble in the reaction solvent are isolated by evaporation of the solvent. Compounds of Formula I then may be purified by trituration of the evaporation residue with solvents such as 1-chlorobutane or ethyl ether and filtration, by recrystallization from mixtures of solvents such as 1,2-dichloroethane, 1-chlorobutane, and heptane, or by chromatography on silica gel.

Many of the compounds of Formula I can be prepared by the procedure shown in Equation 2, where Y, R, R₁, and R₂ are as previously defined. ##STR12##

The reaction shown in Equation 2 is carried out by contacting phenyl carbamates of Formula (3) with aminoheterocycles of Formula (2) in an inert organic solvent such as dioxane or tetrahydrofuran at temperatures of about 20°-100° C. for a period of about one-half to twenty-four hours. The product can be isolated by evaporation of the reaction solvent and purified by methods previously described.

Phenyl carbamates of Formula (3) can be prepared by the methods described, or modifications thereof known to those skilled in the art, in European patent application 44,808, published Jan. 27, 1982; or South African patent application 82/5042.

Alternatively, many of the compounds of Formula I can be prepared by the method described in Equation 3, where Y, R₁, and R₂ are as previously defined and R is H. ##STR13##

The reaction of Equation 3 can be carried out by contacting equimolar amounts of a sulfonamide of Formula (4) with a heterocyclic phenyl carbamate of Formula (5) in the presence of an equimolar amount of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), by methods analogous to those described in South African patent application 83/0441. The phenyl carbamate of Formula (5) can be prepared by methods, or modifications thereof known to those skilled in the art, described in South African patent application 82/5671 and South African patent application 82/5045.

The unsubstituted and substituted alkoxy, allyloxy and propargyloxy benzenesulfonamide intermediates of Formula (4a) can be prepared by one or more of the following general methods.

As shown in Equation 4, one highly useful general route starts from the phenol (6). ##STR14## where R₁ is as previously defined, and R₃ is alkyl, haloalkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkoxyalkyl, alkylthioalkyl, haloalkylthioalkyl, alkylsulfinylalkyl, haloalkylsulfinylalkyl, alkylsulfonylalkyl, haloalkylsulfonylalkyl, or cyanoalkyl. M₁ is Na or K. X₁ is Cl, Br, I, ##STR15##

A solution or suspension of 4-hydroxy-2-nitrobenzoic acid (6) in a suitable polar aprotic solvent, such as dichloromethane or N,N-dimethylformamide (DMF), is treated with at least two equivalents of R₂ X₁ (7) in the presence of at least two equivalents of a suitable base such as N,N-diisopropylethylamine or potassium carbonate and at a temperature between 20° and 155° C. for four to sixteen hours (Equation 4a). If the solvent is miscible with water, it is then evaporated, and the residue is taken up in dichloromethane. The product solution is washed with aqueous sodium or potassium carbonate solution and aqueous hydrochloric acid, and then is dried over a suitable desiccant such as magnesium sulfate. Filtration and evaporation of the solvent leaves (8) in semipurified form. It may be further purified through recrystallization or chromatography on a column of silica gel. The requisite alkylating, alkenylating, and alkynylating agents R₃ X₁ (7) are either known or may be made by a wide variety of methods known in the art.

In cases where R₃ is not the same as R₁, the ester (8) is treated with at least one equivalent of sodium or potassium hydroxide in a mixture of water and a suitable organic cosolvent such as ethanol or p-dioxane at a temperature between 20° and 100° C. for four to sixteen hours (Equation 4b). The reaction mixture is then acidified with concentrated hydrochloric acid. If the product separates out in crystalline form, it is collected. Otherwise the aqueous solution is extracted with ether. The ether solution is dried over sodium sulfate and filtered, and the solvent is evaporated to afford the carboxylic acid (10).

To convert carboxylic acid (10) to ester (12), a solution of it in pyridine is treated sequentially with p-toluenesulfonyl chloride and R₁ OH (11) according to the general procedure of J. H. Brewster and C. J. Ciotti, Jr., J. Am. Chem. Soc. 1955, 77, 6214.

Alternatively, the carboxylic acid (10) may be converted to ester (12) through the use of excess R₁ OH (11) and a strong acid catalyst such as hydrogen chloride as reviewed by C. A. Buehler and D. E. Pearson, Survey of Organic Syntheses, Wiley-Interscience, New York, 1970, pp 802-807 (Equation 4c).

The nitrobenzene (12) is reduced to the aniline (13) either by use of iron in acetic acid as reviewed by C. A. Buehler and D. E. Pearson (ibid, pp 413-414) or by hydrogenation using platinum sulfide as catalyst and the conditions of F. S. Dovel and H. Greenfield, J. Am. Chem. Soc., 87, 2767 (1965) (Equation 4d). When the other substituents present are not potentially susceptible to hydrogenation of hydrogenolysis, palladium may replace platinum sulfide as catalyst.

The aniline (13) is converted to the sulfonyl chloride (14) using the general procedures of H. Meerwein, G. Dittmar, R. Gollner, K. Hafner, F. Mensch, O. Steinfort, Chem. Ber., 90, 841 (1957) (Equation 4e). To limit the hydrolysis of the product during the coupling step, the use of dichloromethane as a cosolvent is advantageous.

Finally, the sulfonyl chloride (14) is aminated to give (4a) using two equivalents of ammonia in dichloromethane solution at a temperature between -30° and -10° C. (Equation 4f).

Alternatively, many of the sulfonamides (4a) can be prepared via a route shown in Equation 5 starting from 2,4-dihydroxybenzoic acid (15). ##STR16## where M₁, R₁, and X₁ are as previously defined and R₃ is alkyl, haloalkyl, alkoxyalkyl, haloalkoxyalkyl, alkylsulfonylalkyl, haloalkylsulfonylalkyl, or benzyl.

Phenol (15) is added to a solution of two equivalents of sodium in anhydrous methanol, ethanol, or amyl alcohol. A little more than one equivalent of R₃ X₁ (7) is added and the mixture is heated at reflux for 4 to 24 hours. The solvent is removed in vacuo and the residue is partitioned between 1N hydrochloric acid and ether. The ether phase is dried over sodium sulfate, and filtered. Evaporation of the ether leaves the phenol (16) (Equation 5a).

The carboxylic acid (16) is converted to ester (17) through the use of excess R₁ OH and a strong acid catalyst such as hydrogen chloride as reviewed by C. A. Buehler and D. E. Pearson (op.cit., pp 802-807) (Equation 5b).

The phenol (17) is converted to the thiocarbamate (18) through the use of dimethylthiocarbamoyl chloride and 1,4-diazabicyclo[2.2.2]octane (DABCO) in N,N-dimethylformamide according to the general procedure of M. S. Newman and H. A. Karnes, J. Org. Chem. 1966, 31, 3980 (Equation 5c). Alternatively a mixture of the phenol (17), at least one equivalent of dimethylthiocarbamoyl chloride, at least one equivalent of triethylamine (Et₃ N), and a catalytic amount of 4-dimethylaminopyridine (DMAP) in dichloromethane is heated at reflux for one to seven days. The reaction mixture is washed with 1N hydrochloric acid and 10% aqueous sodium hydroxide solution, then dried over magnesium sulfate and filtered. Evaporation of the solvent leaves crude (18) which may be purified by chromatography on silica gel or by recrystallization if it is crystalline.

The thiocarbamate (18) is converted to its isomer (19) by heating according to the general procedure of M. S. Newman and H. A. Karnes (op.cit.) (Equation 5d).

To a solution of (19) in anhydrous R₁ OH (11) is added little more than one equivalent of NaOR₁ (20). The mixture is heated at 60°-70° C. for 0.5-1 hour. The solvent is removed in vacuo, and the residue is partitioned between dichloromethane and water. The aqueous phase is washed with dichloromethane, acidified with 12N hydrochloric acid, and extracted with dichloromethane. The dichloromethane extracts are dried over sodium sulfate and filtered. Evaporation of the solvent leaves thiol (21) (Equation 5e).

To a mixture of the thiol (21) and at least one equivalent of sodium formate in formic acid is added at least three equivalents of hydrogen peroxide at such a rate as to keep the temperature between 40° and 50° C. The reaction mixture is then heated at 45°-55° C. for 1 to 5 hours. The excess peroxide is destroyed with sodium sulfite, and the solvent is evaporated. The residue is added to excess thionyl chloride, and a catalytic amount of N,N-dimethylformamide (DMF) is added. The mixture is heated at reflux for 8 to 24 hours, and then the solvent is evaporated. The residue is partitioned between water and ether. The ether solution is washed with aqueous sodium bicarbonate solution, dried over magnesium sulfate and filtered. Evaporation of the solvent leaves the sulfonyl chloride (14) (Equation 5f).

Finally the sulfonyl chloride (14) is aminated giving the sulfonamide (4a) as already described for Equation 4f (Equation 5g).

Most of the sulfonamides (4a) can be prepared via the route shown in Equation 6 starting from 6-hydroxysaccharin (22). ##STR17## where M₁, R₁, and X₁ are as previously defined, X₂ is F, Cl, Br or I, and R₃ is alkyl, haloalkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkoxyalkyl, alkylthioalkyl, haloalkylthioalkyl, alkylsulfinylalkyl, haloalkylsulfinylalkyl, alkylsulfonylalkyl, haloalkylsulfonylalkyl, or aminoalkyl.

6-Hydroxysaccharin (22) can be prepared as described by C. Finzi and M. Colonna, Atti. accad. Lincei, Classe, sci, fis., mat. mat., 1937, 26, 19 (Chem. Abst. 1938, 32, 3762). Alternatively, (4a), where R₁ =CH₃, R₃ =C₆ H₅ CH₂ may be prepared via the route described by Equation 5. A solution of this sulfonamide in dichloromethane is treated with one equivalent of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU). The solvent is evaporated, and the residue is dissolved in minimal water and acidified with concentrated hydrochloric acid to precipitate 6-benzyloxysaccharin. This is dissolved in ethanol containing palladium catalyst. The mixture is hydrogenated at 20°-40° C. and 1-10 psi until hydrogen uptake ceases. Filtration and evaporation of the solvent affords 6-hydroxysaccharin (22).

In the method described by Equation 6a, 6-hydroxysaccharin (22) is added to a solution of two equivalents sodium in anhydrous methanol, ethanol, or amyl alcohol. A little more than one equivalent of R₃ X₁ (7) is added and the mixture is heated at reflux for 4 to 24 hours. The solvent is removed in vacuo and the residue is dissolved in minimal water. It is acidified with concentrated hydrochloric acid. If the product crystallizes, it is collected, washed with dilute hydrochloric acid, and dried. If it does not crystallize, the aqueous mixture is extracted with dichloromethane. The dichloromethane phase is dried over sodium sulfate and filtered. Evaporation of the solvent leaves the saccharin (23) (Equation 6a).

Alternatively, in many cases the saccharin (23) may be prepared by treating a halosaccharin (30) in a polar aprotic solvent such as N,N-dimethylformamide at 20° to 150° C. (90° C. is typical) with at least two equivalents of the corresponding alkoxide of Formula (23.1) until the reaction is done (typically 18 hours). The reaction is worked up by evaporation of the solvent. The residue is dissolved in minimal water and acidified with concentrated hydrochloric acid. If the saccharin (23) crystallizes, it is filtered. Otherwise the aqueous solution is extracted with dichloromethane, and evaporation of the solvent leaves the saccharin (23) (Equation 6a.1).

A solution or suspension of the saccharin (23) in R₁ OH (11) is saturated with hydrogen chloride. The mixture is heated at 65°-80° C. for 1-6 hours. The solvent and hydrogen chloride are evaporated. The residue is dissolved in dichloromethane, washed with aqueous sodium bicarbonate solution, dried over sodium sulfate, and filtered. Evaporation of the solvent affords the sulfonamide (4a) (Equation 6b).

Alternatively, saccharin (22) may be opened to the sulfonamide (24) using the conditions already described for the conversion of (23) to (4a) in Equation 6b (Equation 6c). To a solution of the sulfonamide (24) in anhydrous methanol, ethanol, amyl alcohol, or a suitable aprotic solvent such as N,N-dimethylformamide is added one equivalent of sodium or potassium methoxide, ethoxide, or tert-butoxide followed by the alkylating agent R₃ X₁ (7). The mixture is held at 20°-80° C. for 1-8 hours. The solvent is removed in vacuo, and the residue is dissolved in dichloromethane, washed with aqueous sodium bicarbonate solution, dried over Na₂ SO₄, and filtered. Evaporation of the solvent affords the sulfonamide (4a) (Equation 6d).

Sulfonamides of Formula (4b) can be prepared by the method shown in Equation 7. ##STR18## where M₁, R₁ and X₁ are as previously defined, X₂ is F, Cl, Br or I, and R₄ is alkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkoxyalkyl, alkylthioalkyl, or haloalkylthioalkyl.

The hydroxysaccharin (22) is converted to the thiocarbamate (25) through the use of dimethylthiocarbamoyl chloride and 1,4-diazabicyclo[2.2.2]octane (DABCO) in N,N-dimethylformamide according to the general procedure, or modifications thereof known to those skilled in the art, of M. S. Newman and H. A. Karnes (op.cit.) (Equation 7a).

The thiocarbamate (25) is converted to its isomer (26) by heating according to the general procedure, or modifications thereof known to those skilled in the art, of M. S. Newman and H. A. Karnes (ibid.) (Equation 7b).

To a solution of (26) in anhydrous methanol is added a little more than two equivalents of sodium methoxide. The mixture is heated at 60°-70° C. for 0.5-1 hour. The solvent is removed in vacuo, and the residue is partitioned between dichloromethane and water. The aqueous phase is washed with dichloromethane and acidified with concentrated hydrochloric acid. If the saccharin (27) crystallizes, it is collected, rinsed with dilute cold hydrochloric acid, and dried. If it does not crystallize, the aqueous phase is extracted with dichloromethane. The dichloromethane extracts are dried over sodium sulfate and filtered. Evaporation of the solvent leaves saccharin (27) (Equation 7c).

The mercaptan (27) is added to a solution of two equivalents sodium in anhydrous methanol, ethanol, or amyl alcohol. A little more than one equivalent of R₄ X₁ (28) is added, and the mixture is heated at reflux for 1 to 8 hours. The requisite alkylating, alkenylating, and alkynylating agents R₄ X₁ (28) are either known in the art or may be made by a wide variety of methods known in the art.

The solvent is removed in vacuo, and the residue is dissolved in minimal water. It is acidified with concentrated hydrochloric acid. If the saccharin (29) crystallizes, it is collected, washed with cold dilute hydrochloric acid, and dried. If it does not crystallize, the aqueous mixture is extracted with dichloromethane. The dichloromethane phase is dried over sodium sulfate and filtered. Evaporation of the solvent leaves the saccharin (29) (Equation 7d).

Alternatively, in many cases, the saccharin (29) may be prepared by treating a halosaccharin (30) in a polar aprotic solvent such as N,N-dimethylformamide at 20°-100° C. with at least two equivalents of the corresponding thiolate of Formula (31) for 1-24 hours. The reaction is worked up by evaporation of the solvent. The residue is dissolved in minimal water and acidified with concentrated hydrochloric acid. If the saccharin (29) crystallizes, it is filtered. Otherwise the aqueous solution is extracted with dichloromethane, and evaporation of the solvent leaves the saccharin (29) (Equation 7e).

The requisite precursor halosaccharins of Formula (30) may be prepared by conversion of the corresponding 4-halo-2-nitrobenzoic acids to esters of 2-(amino-sulfonyl)-4-halobenzoic acids by use of methods analogous to those described for Equation 4. These esters are closed to the corresponding saccharins of Formula (30) by treatment with DBU according to the general method already described for the preparation of 6-benzyloxysaccharin.

The saccharin (29) is then opened to the sulfonamide (4b) using the conditions already described for the conversion of (23) to (4a) in Equation 6b (Equation 7f).

Alternatively, saccharin (27) may be opened to the sulfonamide (32) using the conditions already described for the conversion of (23) to (4a) in Equation 6b (Equation 7g). The thiol (32) is then converted to (4b) using the method already described for the conversion of (24) to (4a) in Equation 6d (Equation 7h).

Sulfonamides of Formula (4c) can be prepared by the method shown in Equation 8. ##STR19## where R₁ is as previously defined; R₅ is alkyl, cyclopropyl, haloalkyl, alkoxyalkyl, haloalkoxyalkyl, alkylsulfonylalkyl, haloalkylsulfonylalkyl, haloalkoxy, alkenyl or alkynyl; R₆ is alkyl or haloalkyl; and R₇ is alkyl, cyclopropyl, haloalkyl, alkoxyalkyl, haloalkoxyalkyl, alkylthioalkyl, haloalkylthioalkyl, alkylsulfinylalkyl, haloalkylsulfinylalkyl, alkylsulfonylalkyl, haloalkylsulfonylalkyl, haloalkoxy, alkenyl or alkynyl. M₂ is Na or K.

The starting nitrobenzenes (33) are either known in the art or may be made by a wide variety of methods known in the art. Some of these methods include the nitration (for a review, see G. Lehmann. H. Eichmann "Formation of Carbon-Nitrogen Bonds" in Preparative Organic Chemistry, G. Hilgetag, A. Martini ed., Wiley-Interscience, New York, 1972) of the coupling product obtained from reaction of the appropriate halide with diphenylcuprate (for a review, see G. H. Posner "Substitution Reactions Using Organo-copper Reagents" in Organic Reactions, Vol. 22, W. G. Dauben ed., Wiley, New York, 1975).

Another method is the Friedel-Crafts acylation of benzene with the appropriate acid halide or anhydride (for a review, see G. A. Olah, Friedel-Crafts and Related Reactions, Volumes I-IV, Wiley-Interscience, New York, 1963-1965), followed by reductive removal of the carbonyl oxidation (for a review, see C. Bischoff, P.-G. Dietrich, E. Hoft, D. Murowski, "Formation of Carbon-Hydrogen Bonds" in Preparative Organic Chemistry, G. Hilgetag, A. Martini ed., Wiley-Interscience, New York, 1972) and then nitration.

Still another method involves conversion of the appropriate 4-nitrobenzyl alcohols, aldehydes, or ketones to their mono or difluoro alkyl homologues using the conditions reviewed by G. A. Boswell, Jr., W. C. Ripka, R. M. Scribner, C. W. Tullock, "Fluorination by Sulfur Tetrafluoride" and C. M. Sharts, W. A. Sheppard "Modern Methods to Prepare Monofluoroaliphatic Compounds" in Organic Reactions, Vol. 21, W. G. Dauben ed., Wiley, New York, 1974).

The nitrobenzene (33) is reduced to the aniline (34) using the conditions already described for the conversion of (12) to (13) in Equation 4d (Equation 8a).

The aniline (34) in a suitable solvent such as benzene is treated with at least one equivalent of acetic anhydride and heated at reflux for 8-24 hours. The reaction mixture is cooled, and if the acetanilide (35) crystallizes, it is collected and dried. If it does not crystallize, the benzene solution is washed with 1N hydrochloric acid and aqueous sodium bicarbonate solution, dried over magnesium sulfate, and filtered. Evaporation of the solvent leaves the acetanilide (35) (Equation 8b).

The acetanilide (35) is then nitrated using the general conditions reviewed by G. Lehmann and H. Teichmann (op.cit.) to give nitroacetanilide (36) (Equation 8c).

A slurry of acetanilie (36) in 1N hydrochloric acid is heated at reflux until all of the solid dissolves. The solution is then made slightly basic with sodium bicarbonate and is extracted with dichloromethane. The dichloromethane extracts are dried over sodium sulfate and filtered. Evaporation of the solvent leaves the aniline (37) (Equation 8d).

As the nitric acid used in the reaction depicted by Equation 8c can act as an oxidizing agent, substituent R₅ of aniline (37) cannot contain an alkylthio, haloalkylthio, alkylsulfinyl, or haloalkylsulfinyl group. But R₅ can be all of the other substituents allowed for R₇ that do not contain an alkylthio, haloalkylthio, alkylsulfinyl, or haloalkylsulfinyl group. In these cases the reaction depicted by Equation 8e is skipped, and aniline (39) used in Equation 8f is prepared as aniline (37).

On the other hand in those cases where R₇ does contain an alkylthio, haloalkylthio, alkylsulfinyl, or haloalkylsulfinyl group, the alkylthio-, haloalkylthio-, alkylsulfinyl-, or haloalkylsulfinyl-containing aniline (39) is prepared from a homologous aniline (37) having a R₅ substituent containing a displaceable halogen atom at the position where the lower valent sulfur-containing group is to be placed. To effect the displacement of the halogen by an alkylthio or haloalkylthi group, a solution of halide (35) in a suitable solvent such as N,N-dimethylformamide is treated with a little more than one equivalent of the appropriate sodium or potassium alkylthiolate or haloalkylthiolate (38). The mixture is held at 20°-100° C. for 1-8 hours. The solvent is then evaporated, and the residue is partitioned between water and dichloromethane. The dichloromethane solution is dried over sodium sulfate and filtered. Evaporation leaves the alkylthio or haloalkylthio compound (39) respectively.

When the appropriate haloalkylthiolate reagent (38) is unstable to self-condensation, the corresponding hydroxy-, carbonyl-, and/or carboxy-containing alkylthiolate reagent can be used. After formation of the thioether bridge, these oxygen-containing groups can be converted to the desired halogen substitution pattern by use of a wide variety of methods known in the art.

Anilines of Formula (39) where R₇ contains an alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, or haloalkylsulfonyl group can be prepared by oxidation of the corresponding alkylthio- or haloalkylthio-containing anilines using methods analogous to those described for the conversion of (4b) to (4d) in Equation 9 (Equation 8e).

The aniline (39) is then diazotized and subjected to the Sandmeyer reaction according to the general experimental procedure of G. T. Morgan and E. A. Coulson, J. Chem. Soc. 1929, 2551 to give nitrile (40) (Equation 8f).

A suspension of the nitrile (40) in 75-80% aqueous sulfuric acid is heated at 95°-100° C. for 2-5 hours. Then over 1-2 hours and at a temperature of 80°-100° C. 1.5-2.5 equivalents of sodium nitrite is added in small portions. The heating is continued 0.5-1 hour longer, then the mixture is cooled and poured onto excess ice. If the carboxylic acid (41) crystallizes, it is collected, rinsed with ice water and dried. If it does not crystallize, the aqueous mixture is extracted with dichloromethane. The dichloromethane solution is extracted with aqueous 10% sodium carbonate solution. The aqueous extract is made acidic with concentrated hydrochloric acid. If the carboxylic acid (41) then crystallizes, it is collected, rinsed with ice water and dried. If it does not crystallize, the aqueous solution is extracted with ether. The ether extracts are dried over magnesium sulfate and filtered. Evaporation of the solvent leaves carboxylic acid (41) (Equation 8g).

By use of the methods previously described, carboxylic acid (41) can be converted to sulfonamide (4c) (Equation 8h).

Sulfonamides of Formula (4c) where R₇ is alkyl substituted with an alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, or haloalkylsulfonyl group can be prepared by peracid oxidation of the corresponding sulfonamides of Formula (4c) where R₇ is alkyl substituted with an alkylthio or haloalkylthio group using methods analogous to those described for the preparation of sulfinyl sulfonamides of Formula (4d, n=1) and sulfonyl sulfonamides of Formula (4d, n=2) in Equation 9 (vide infra).

The sulfinyl sulfonamides of Formula (4d, n=1) and sulfonyl sulfonamides of Formula (4d, n=2) can be be prepared from the corresponding thio sulfonamides of Formula (4b) as shown in Equation 9. ##STR20## where R₁ and R₄ are as previously defined and n is 1 or 2.

To prepare the sulfinyl sulfonamides of Formula (4d, n=1) a solution of one equivalent of a peracid, such as 3-chloroperoxybenzoic acid, in an inert solvent, such as dichloromethane, is added to a stirred solution of the appropriate thio sulfonamide (4b) in an inert solvent, such as a mixture of dichloromethane and tetrahydrofuran, at 0°-5° C. The mixture is then warmed to 20°-40° C. When thin layer chromatography has revealed the sulfonamide (4b) to have been oxidized, the mixture is washed in turn with 5% aqueous sodium sulfite solution, saturated aqueous sodium bicarbonate solution, water, and brine, and then dried (MgSO₄). Evaporation of the solvent then leaves the sulfinyl sulfonamide of Formula (4d, n=1).

To prepare sulfonyl sulfonamide of Formula (4d, n=2) a solution of more than two equivalents (only two equivalents when R₄ is alkenyl or alkynyl) of a peracid, such as 3-chloroperoxybenzoic acid, in an inert solvent, such as 1,2-dichloroethane, is added to a stirred mixture of the appropriate thio sulfonamide (4b) in an inert solvent, such as 1,2-dichloroethane, containing 1-5 mol % of a free radical inhibitor, such as 4,4-thiobis(6-tert-butyl-m-cresol). The mixture is heated to 50°-80° C. When thin layer chromatography shows the thio sulfonamide (4b) and intermediate sulfinyl sulfonamide (4d, n=1) to have been consumed, the mixture is cooled and diluted with tetrahydrofuran to maintain sulfonamide solubility. Using the same work up method as already described for the preparation of sulfinyl sulfonamides (4d, n=1), one obtains the sulfonyl sulfonamides of Formula (4d, n=2).

The amino sulfonamides of Formula (4e) are prepared as shown in Equation 9.1 and discussed below. ##STR21## where R₁ and X₂ are as previously defined, R_(b) ' is H or alkyl, and R_(c) ' is H, alkyl, or haloalkyl.

In most cases the amino saccharins of Formula (41.2) are prepared by treating halo saccharins of Formula (30) with one or more equivalents of the corresponding amine derivatives of Formula (41.1) using one or more of a wide variety of experimental conditions known in the art. In some cases the reaction can be run using an excess of the amine derivative (41.1) as the only solvent and heating the mixture to 30°-200° C. at atmospheric pressure or, if the boiling point of the amine derivative makes necessary, at above atmospheric pressure. In other cases the use of a polar inert solvent such as N,N-dimethylformamide is advantageous. When the amine derivative is itself difficult or expensive to prepare, the amount of it used can be reduced to little more than one equivalent if at least one equivalent of another base such as triethylamine, N,N-diisopropyl-N-ethylamine, diazabicyclo[5.4.0]undec-7-ene, sodium hydride, or n-butyllithium is added to the reaction mixture. Besides reducing the amount of amine derivative needed, the use of at least two equivalents of very strong bases, such as n-butyllithium or sodium hydride, capable of deprotonating the amine derivative can accelerate the rate of the displacement reaction and allow it to proceed at lower temperatures as is well known in the art. The requisite amine derivatives (41.1) are either known or can be made by methods known in the art.

After the displacement reaction is complete the solvent and excess of any volatile amine derivative (41.1) is evaporated and the residue is dissolved in 5% aqueous sodium hydroxide solution. Concentrated hydrochloric acid is added until the pH is 7. If the saccharin (41.2) crystallizes, it is filtered. Otherwise the aqueous solution is saturated with salt and then extracted with dichloromethane, and in most cases evaporation of the dichloromethane leaves the saccharin (41.2). If it does not, the aqueous solution is evaporated to dryness and the residue is continuously extracted with tetrahydrofuran. Evaporation of the solvent then leaves the saccharin (41.2) (Equation 9.1a).

In some cases saccharins of Formula (41.2) may be prepared from saccharins of Formula (41.2) having fewer substituents on the amino group. A variety of methods are well-known in the art for the alkylation of aniline amino groups and their derivatives.

To prepare the sulfonamide of Formula (4e) a solution or suspension of the saccharin (41.2) in the appropriate alcohol R₁ OH (11) is saturated with hydrogen chloride. The mixture is heated at 65°-80° C. for 1-12 hours. The solvent and hydrogen chloride are evaporated. The residue is dissolved in a mixture of brine and 5:1 (vol.) dichloromethane-tetrahydrofuran. Sodium carbonate is added to the vigorously stirred mixture until it is made basic. The dichloromethane-tetrahydrofuran phase is then separated, and evaporation of the solvent leaves the sulfonamide of Formula (4e) (Equation 9.1b).

Sulfonyl isocyanates (1) are prepared from the corresponding sulfonamides (4) with compatible R₂ substituents by one of the following two general methods. ##STR22## where R₁ and R₂ are as previously defined.

The sulfonamide (4) and an alkyl isocyanate (e.g. n-butyl isocyanate) in xylene or other solvent boiling above 135° C. are mixed in the presence or absence of a catalytic amount of 1,4-diaza[2.2.2]bicyclooctane (DABCO) and heated to 135°-140° C. After 5-60 minutes phosgene is slowly added to the heated mixture at such a rate that the temperature remains between 133°-135° C. When the consumption of phosgene has ceased, the mixture is cooled and filtered to remove insoluble material. Finally, the solvent, alkyl isocyanate, and excess phosgene are evaporated, leaving the sulfonyl isocyanate (1).

If desired, the alkyl isocyanate-sulfonamide adduct can be made and isolated before reaction with the phosgene. In this case, the sulfonamide (4), alkyl isocyanate, and anhydrous base (e.g., K₂ CO₃) in a polar, aprotic solvent (e.g. acetone, butanone, or acetonitrile) are mixed and heated under reflux for 1 to 6 hours. The reaction mixture is then diluted with water, and the pH is adjusted to about 3 with acid (e.g. HCl, H₂ SO₄). The adduct is filtered out and dried, and then reacted with phosgene as described above. This procedure modification is especially useful when sulfonamide (4) is high melting and has low solubility in the phosgenation solvent.

Sulfonyl isocyanates (1) can also be prepared by the following method. ##STR23## where R₁ and R₂ are as previously defined and (4) is (4a), (4b), (4c) or (4d).

The sulfonamide (4) is heated at reflux in an excess of thionyl chloride. The reaction is continued until the sulfonamide protons are no longer detectable in the proton magnetic resonance spectrum. From 16 hours to 5 days is typically sufficient for complete conversion to the thionylamide (42) (Equation 11a).

The thionyl chloride is evaporated and the residue is treated with an inert solvent (e.g. toluene) containing at least one equivalent (typically 2-3 equivalents) of phosgene. A catalytic amount of pyridine (typically 0.1 equivalent) is added, and the mixture is heated to about 60°-140° C. with 80°-100° preferred. Conversion to the isocyanate (1) is usually substantially complete within 15 minutes to 3 hours (Equation 11b). The mixture is then cooled and filtered, and the solvent is evaporated, leaving the sulfonyl isocyanate (1).

The heterocyclic amines of Formula (2a) to (2c) below are taught in U.S. Pat. No. 4,478,635. ##STR24##

In some cases, heterocycles of Formula (2) may be more easily prepared with R being H than with R being CH₃. Many heterocycles (2, R═CH₃) can be prepared from the corresponding heterocycles (2, R═H) by one or more of the following two methods. ##STR25## where A is ##STR26## and Y is as previously defined.

In this method, a solution or slurry of the appropriate heterocycle (2, R═H) in a suitable aprotic solvent (e.g., tetrahydrofuan, dioxane, glyme) at 0°-30° C. is treated with two equivalents of sodium hydride. After gas evolution ceases, the reaction mixture is treated with one equivalent of dimethyl carbonate and stirred at 20°-30° C. for 8 to 24 hours to provide a suspension of the sodium salt (43) (Equation 12a).

The reaction mixture containing (43) is treated with at least two equivalents of iodomethane and then heated at 60°-80° C. for 8 to 24 hours. The mixture is cooled and filtered, and the solvent is evaporated. The residue is taken up in dichloromethane, washed with water, and the solvent is evaporated, leaving the N-methyl carbamate (44, R═CH₃) (Equation 12b).

The carbamate (44, R═CH₃) is dissolved in anhydrous, alcohol-free chloroform saturated with propylene gas. Slightly more than one equivalent (typically 1.1-1.2 equivalents) of iodotrimethylsilane) is added and the stirred solution is heated at 50°-60° C. for 2 to 4 hours. The mixture is cooled and two equivalents of methanol is added. The solvent is evaporated and the residue is taken up in methanol. The mixture is carefully neutralized with 10% sodium methoxide in methanol, and then the solvent is evaporated. The residue is triturated with ice water. If a precipitate forms, it is filtered out, rinsed with ice water and dried to provide (2, R═CH₃). If no precipitate forms, the solution is saturated with sodium chloride and extracted with ethyl acetate. Evaporation of the solvent leaves heterocycle (2, R═CH₃) (Equation 12c).

Alternatively, the following two-step procedure is useful in many cases. ##STR27## where A is as previously defined.

A solution of the amine (2, R═H) in concentrated hydrochloric acid is treated with sodium nitrite solution and the chloro compound (45) is isolated in the usual manner by filtration of the acidic solution (Equation 13a). A representative procedure is described by Bee and Rose in J. Chem. Soc. C. 1966, 2031.

The heterocycle (45) is then treated with at least two equivalents of methylamine in a suitable inert solvent (e.g. tetrahydrofuran, glyme, or diglyme) at a temperature between 20° and 80° C. for 1-18 hours (Equation 13b). The reaction mixture is then cooled and filtered. Evaporation of the solvent leaves (2, R═CH₃) contaminated with a little CH₃ NH₃ ⁺ Cl⁻ salt. The product may be purified by trituration with ice water or by dissolution in dichloromethane, followed by washing with a small amount of water, drying, and evaporation of solvent. Further purification may be accomplished by recrystallization or column chromatography on silica gel.

As an alternative to the methods already described in which the sulfonamides of Formulae (4a), (4b), (4d), and (4e) are fully elaborated prior to construction of the urea bridge of compounds of Formula I, many compounds of Formula Ia may be prepared by the method described in Equation 14. ##STR28## where R₁, X₁ and Y are as previously defined, W is O, NR_(b) ' or S, and R₈ is alkyl, haloalkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkoxyalkyl, alkylthioalkyl, haloalkylthioalkyl, alkylsulfinylalkyl, haloalkylsulfinylalkyl, alkylsulfonylalkyl, haloalkylsulfonylalkyl, or cyanoalkyl when W is O; R₈ is alkyl, haloalkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkoxyalkyl, alkylthioalkyl, haloalkylthioalkyl, or cyanoalkyl when W is S; and R₈ is alkyl or haloalkyl when W is NR_(b) ' (R_(b) ' is as previously defined).

In this method a solution of the appropriate compound of Formula (46) in a polar solvent such as a mixture of acetonitrile and N,N-dimethylformamide is treated with two equivalents of a strong base such as sodium methoxide or sodium hydride with catalytic methanol followed by a little more than one equivalent of the appropriate alkylating, alkenylating, or alkynylating agent (47). The mixture is held at 20°-60° C. for 2-24 hours. Then the mixture is poured into excess hydrochloric acid. If the compound of Formula Ia crystallizes, it is filtered. Otherwise the aqueous mixture is extracted with dichloromethane, and evaporation of the solvent leaves the compound of Formula Ia. The compounds of Formula (46) are in turn prepared by coupling the appropriate sulfonamides of Formulae (24) (W═O), (32) (W═S), or (4e) (R_(c) '═H) (W═NR_(b) ') with the appropriate heterocyclic phenyl carbamates of Formula (5,R═H) according to the general method described for Equation 3.

Many of the compounds of Formula Ia where R₈ is alkyl, haloalkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkoxyalkyl, or cyanoalkyl and W is S(O) or S(O)₂ can be made by oxidation of the corresponding compounds of Formula Ia where W is S using methods similar to those already described for the conversion of (4b) to (4d) in Equation 9.

The following examples further illustrate the synthesis of this invention.

EXAMPLE 1 Methyl 4-ethoxy-2-hydroxybenzoate

Hydrogen chloride was bubbled into a stirred solution of 4-ethoxy-2-hydroxybenzoic acid (101.0 g, 0.554 mol) in methanol (2000 mL) until the solution was saturated. The solution was heated under reflux for 3 days and then cooled to 15° C. This caused the product to crystallize out. The crystals were collected, rinsed with methanol and hexanes, and dried. Methyl 4-ethoxy-2-hydroxybenzoate was obtained as a pale amber solid (49.3 g) melting at 77°-78° C.

PMR (CDCl₃, 90 MHz): δ11.90 (slightly broadened s, 1H, OH); 7.76 (d, 1H, H ortho to CO₂ CH₃): 6.35-6.55 (m, 2H, other aryl H's): 4.06 (q, 2H, OCH₂ CH₃); 3.89 (s, 3H, OCH₃): 1.41 (t, 3H, OCH₂ CH₃). IR (Nujol); 3130 (broad, w, OH): 1668 (s, C═O) cm⁻¹. More product was obtained by reworking the mother liquor.

EXAMPLE 2 Methyl 2-[(dimethylamino)thioxomethoxy]-4-ethoxybenzoate

Triethylamine (76.6 mL, 0.550 mol) was added via syringe to a stirred solution of methyl 4-ethoxy-2-hydroxybenzoate (49.3 g, 0.251 mol), 4-dimethylaminopyridine (3.06 g, 0.025 mol), and dimethylthiocarbamoyl chloride (54.4 g, 0.440 mol) in dry dichloromethane (411 mL). The reaction solution was heated at reflux three days and then allowed to stand at room temperature overnight. It was washed with hydrochloric acid (1N, 3×300 mL) and then dried (MgSO₄) and filtered. Rotary evaporation of the solvent left crude product (95.2 g) as a brown oil. This was applied to a column of silica gel and eluted with 2:1 followed by 1:1 hexanes-ether. Fractions containing product (R_(f) =0.43, 1:1 hexanes-ether, UV) were rotary evaporated to give partially purified product (60.2 g) as a yellowish solid. Further purification was achieved by additional column chromatography employing a greater silica gel to sample ratio. Finally, the doubly chromatographed product (48.7 g including 7.4 g from another similar run) was recrystallized from boiling methanol (3 mL/g). After cooling in an ice bath, the crystals were collected, rinsed with ice-cold methanol and dried. Methyl 2-[(dimethylamino)thioxomethoxy]-4-ethoxybenzoate was obtained as large white prisms (46.1 g) melting at 77°-79° C.

PMR (CDCl₃, 200 MHz); δ7.96 (d, 1h, H ortho to CO₂ CH₃); 7.81 (dd, 1H, H para to OC(S)N); 6.62 (d, 1H, H ortho to OC(S)N; 4.08 (q, 2H, OCH₂ CH₃); 3.81 (s, 3H, CO₂ CH₃); 3.47 (s, 3H, NCH₃); 3.40 (s, 3H, NCH₃); 1.42 (t, 3H, OCH₂ CH₃). IR (Nujol): 1715 cm⁻¹ (vs. C═O).

EXAMPLE 3 Methyl 2-[(dimethylamino)carbonylthio]-4-ethoxybenzoate

Methyl 2-[(dimethylamino)thioxomethoxy]-4-ethoxybenzoate (28.3 g, 0.100 mol) was heated under nitrogen at 220° C. for 1.5 hours. Thin layer chromatography (6:3:1 CH₃ Cl₂ -hexanes-ether, UV) showed a very faint spot at a R_(f) of 0.63 (starting material) and a very intense spot at a R_(f) of 0.35 (product). In this case the crude product was used in the next reaction step without further characterization or purification.

Crude product from a similar but smaller scale run was chromatographed on a column of silica gel using 4:1 ether-hexanes as eluant. Fractions containing product (R_(f) =0.40, same solvent, UV) were rotary evaporated to give an oil that slowly crystallized. This was dissolved in a little dichloromethane, diluted with 1-chlorobutane, seeded, and rotary evaporated. The residue was collected, rinsed with hexanes, and dried. Methyl 2-[(dimethylamino)carbonylthio]-4-ethoxybenzoate was obtained as white prisms melting at 65°-67° C. PMR (CDCl₃, 200 MHz): δ7.93 (d, 1H, H ortho to CO₂ CH₃); 7.16 (d, 1H, H ortho to SC(O)N); 6.89 (dd, 1H, H para to SC(O)N); 4.08 (q, 2H, OCH₂ CH₃); 3.84 (s, 3H, CO₂ CH₃); 3.09 (broad s, 6H, N(CH₃)₂); 1.42 (t, 3H, OCH₂ CH₃). IR (Nujol): 1730 (s, ester C═O); 1680 (s, carbonyl C═O) cm⁻¹.

EXAMPLE 4 Methyl 4-ethoxy-2-mercaptobenzoate

Methanolic sodium methoxide (4.9M, 22.4 mL, 0.11 mol) was added via syringe to a solution of methyl 2-[(dimethylamino)carbonylthio]-4-ethoxybenzoate (crude, ca. 28.3 g, 0.10 mol) in methanol (100 mL) under nitrogen. The reaction mixture was heated at reflux for 30 minutes, then cooled with the aid of a water bath. Rotary evaporation yielded a solid. This was partitioned between dichloromethane (100 mL) and water (100 mL). The aqueous layer was washed with dichloromethane (3×40 mL), acidified to pH<1 with concentrated hydrochloric acid, and then extracted with dichloromethane (3×40 mL). These dichloromethane extracts were combined, dried (Na₂ SO₄), and filtered. Rotary evaporation yielded methyl 4-ethoxy-2-mercaptobenzoate as an oil (18.4 g) that on standing formed a crystalline solid melting at 42°-44° C. PMR (CDCl₃, 200 MHz); δ7.97 (d, 1H, H ortho to CO₂ CH₃); 6.78 (d, 1H, H ortho to SH); 6.64 (dd, 1H, H para to SH); 5.06 (s, 1H, SH); 4.05 (q, 2H, OCH₂ CH₃); 3.88 (s, 3H, CO₂ CH₃); 1.42 (t, 3H, OCH₂ CH₃). IR (Nujol): 1686 (vs, C═O) cm.sup. -1.

EXAMPLE 5 Methyl 2-(chlorosulfonyl)-4-ethoxybenzoate

Hydrogen peroxide (30%, 9.79M, 30.7 mL, 300 mmol) was added dropwise to a stirred solution of methyl 4-ethoxy-2-mercaptobenzoate (18.2 g, 85.7 mmol) and sodium formate (11.7 g, 172 mmol) in formic acid (171.4 mL). Through the use of an ice bath, the internal temperature was held to 40°-50° C. during the first half of the hydrogen peroxide addition and 45°-50° C. during the second half of the addition. After completion of the addition and cessation of the exothermic reaction, the mixture was heated at 45°-55° C. for two hours. The excess hydrogen peroxide was destroyed with sodium sulfite, the solution was filtered, and the solvent was rotary evaporated. The residue was slurried in toluene and rotary evaporated. The process was repeated to give the sodium sulfonate salt as a moist white crystalline solid (21.7 g).

Without further purification or characterization, the sodium sulfonate salt was added portionwise to stirred thionyl chloride (150 mL, 2.1 mol). Anhydrous N,N-dimethylformamide (1.0 mL, 13 mmol) was added slowly, and the reaction mixture was heated at reflux overnight. The reaction mixture was then rotary evaporated. Dichloromethane (150 mL) was added, and the solvent was again evaporated. The residue was partitioned between ether (100 mL) and ice water (100 mL). The aqueous layer was extracted with ether (2×50 mL). The combined ether solutions were washed with water (50 mL), saturated aqueous sodium bicarbonate solution (2×50 mL), dried MgSO₄), and filtered. Rotary evaporation of the solvent left methyl 2-(chlorosulfonyl)-4-ethoxybenzoate as pale orange oil (22.5 g) that crystallized on scratching. The crystalline solid melted at 45°-48° C. PMR (CDCl₃, 200 MHz): δ7.76 (d, 1H, H ortho to CO₂ CH₃); 7.65 (d, 1H, H ortho to SO₂ Cl); 7.21 (dd, 1H, H para to SO₂ Cl); 4.16 (q, 2H, OCH₂ CH₃); 3.96 (s, 3H, CO₂ CH₃); 1.48 (t, 3H, OCH₂ CH₃). IR (Nujol): 1722 (vs, C═O) cm⁻¹.

EXAMPLE 6 Methyl 2-(aminosulfonyl)-4-ethoxybenzoate

Liquified ammonia (4.4 mL, 180 mmol) was added to a stirred solution of methyl 2-(chlorosulfonyl)-4-ethoxybenzoate (22.1 g, 79.3 mmol) in dichloromethane (221 mL) at -70° C. The reaction mixture was allowed to warm to -10° C. and was held at this temperature for 30 minutes. The mixture was then poured into water (221 mL). More water and dichloromethane were used for rinsing, and tetrahydrofuran (ca. 40 mL) was also added. The layers were shaken and separated, and the aqueous layer was extracted with dichloromethane (2×221 mL). The combined dichloromethane solutions were washed with water (221 mL), and the aqueous wash was back-extracted with dichloromethane (ca. 120 mL). The combined dichloromethane solutions were dried (NaSO₄), and filtered. Rotary evaporation of the solvent left crude product as an off-white crystalline solid (18.1 g). This was dissolved in hot methanol (ca. 200 mL) and hot filtered. The solution was boiled down to a volume corresponding to 3 mL/g methanol. After seeding and cooling with the aid of an ice bath, the crystals were collected, rinsed with ice-cold methanol and hexanes, and dried. Methyl 2-(aminosulfonyl)-4-ethoxybenzoate (15.3g) was obtained as white crystalline needles melting at 146°-148° C. PMR (CDCl₃, 200 MHz): δ 7.91 (d, 1H, H ortho to CO₂ CH₃); 7.68 (d, 1H, H ortho to SO₂ NH₂); 7.04 (dd, 1H, H para to SO₂ NH₂); 5.91 (broad s, 2H, NH₂); 4.14 (q. 2H, OCH.sub. 2 CH₃); 3.95 (s, 3H, CO₂ CH₃); 1.45 (t, 3H, OCH₂ CH₃). IR (Nujol): 3348 (m, NH); 3241 (m, NH); 1692 (s, C═O) cm⁻¹.

EXAMPLE 7 Methyl 2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoate

To a slurry of 4-difluoromethoxy-6-methoxypyrimidin-2-amine (0.56 g, 2.92 mmol) in dry dichloromethane (5 mL) was added a solution of methyl 4-ethoxy-2-(isocyanatosulfonyl)benzoate (crude, ca. 5.6 mL) in dichloromethane (5 mL). The reaction mixture was heated at reflux for 3 hours, during which time the solid dissolved. On stirring at room temperature for 12 hours a new solid formed. The crude reaction mixture was chromatographed directly on a column of silica gel using as eluant 40:1, 20:1, and finally 10:1 dichloromethane-ether, all containing 2 mL/L acetic acid. The appropriate fractions were diluted with toluene and rotary evaporated to give a solid. The solid was slurried in hexanes, collected, washed with butyl chloride, 1:1 butyl chloride-hexanes, hexanes and air dried. The product was a white crystalline solid melting at 195°-196° C. PMR (CDCl₃, 200 MHz): δ 12.02 (bs, 1H); 7.91 (d, 1H); 7.78 (d, 1H); 7.52 (t, 1H); 7.34 (bs, 1H); 7.09 (dd, 1H); 5.97 (s, 1H); 4.17 (q, 2H); 4.12 (s, 3H); 3.87 (s, 3H); 1.46 (t, 3H). IR (Nujol): 1722 (vs, C═O) cm⁻¹.

Using the procedures and examples shown above, the compounds in Tables I-IV can be prepared.

    ______________________________________                                          STRUCTURES FOR TABLES                                                         ______________________________________                                         TABLE I and TABLE Ia                                                                     ##STR29##                                                            TABLE II and TABLE IIa                                                                   ##STR30##                                                            TABLE III and TABLE IIIa                                                                 ##STR31##                                                            TABLE IV and TABLE IVa                                                                   ##STR32##                                                            TABLE Va                                                                                 ##STR33##                                                            TABLE VIa                                                                                ##STR34##                                                            TABLE VIIa                                                                               ##STR35##                                                            TABLE VIIIa                                                                              ##STR36##                                                            ______________________________________                                    

                  TABLE I                                                          ______________________________________                                         R.sub.1 = CH.sub.3                                                             R.sub.2       R       Y          m.p. (°C.)                             ______________________________________                                         Me            H       Me         187-190                                       Me            Me      Me                                                       Me            H       OMe        191-194                                       Me            Me      OMe                                                      Me            H       OCF.sub.2 H                                              Me            Me      OCF.sub.2 H                                              Et            H       Me                                                       Et            Me      Me                                                       Et            H       OMe                                                      Et            Me      OMe                                                      Et            H       OCF.sub.2 H                                              Et            Me      OCF.sub.2 H                                              Pr            H       Me                                                       Pr            Me      Me                                                       Pr            H       OMe                                                      Pr            Me      OMe                                                      Pr            H       OCF.sub.2 H                                              Pr            Me      OCF.sub.2 H                                               .sub.-i-Pr   H       Me                                                        .sub.-i-Pr   Me      Me                                                        .sub.-i-Pr   H       OMe                                                       .sub.-i-Pr   Me      OMe                                                       .sub.-i-Pr   H       OCF.sub.2 H                                               .sub.-i-Pr   Me      OCF.sub.2 H                                              cyclo-Pr      H       Me                                                       cyclo-Pr      Me      Me                                                       cyclo-Pr      H       OMe                                                      cyclo-Pr      Me      OMe                                                      cyclo-Pr      H       OCF.sub.2 H                                              cyclo-Pr      Me      OCF.sub.2 H                                              OMe           H       Me         167-168 d                                     OMe           Me      Me                                                       OMe           H       OMe        172-173                                       OMe           Me      OMe                                                      OMe           H       OCF.sub.2 H                                                                               175-177 d                                     OMe           Me      OCF.sub. 2 H                                             OEt           H       Me         183-184 d                                     OEt           Me      Me                                                       OEt           H       OMe        195-196                                       OEt           Me      OMe                                                      OEt           H       OCF.sub.2 H                                                                               184-185 d                                     OEt           Me      OCF.sub.2 H                                              O-- -n-Pr     H       Me                                                       O-- -n-Pr     Me      Me                                                       O-- -n-Pr     H       OMe                                                      O-- -n-Pr     Me      OMe                                                      O-- -n-Pr     H       OCF.sub.2 H                                              O-- -n-Pr     Me      OCF.sub.2 H                                              O-- .sub.-i-Pr                                                                               H       Me         153-157                                       O-- .sub.-i-Pr                                                                               Me      Me                                                       O-- .sub.-i-Pr                                                                               H       OMe        177-183                                       O-- .sub.-i-Pr                                                                               Me      OMe                                                      O-- .sub.-i-Pr                                                                               H       OCF.sub.2 H                                              O-- .sub.-i-Pr                                                                               Me      OCF.sub.2 H                                              SMe           H       Me         153-156 d                                     SMe           Me      Me                                                       SMe           H       OMe        143-146                                       SMe           Me      OMe                                                      SMe           H       OCF.sub.2 H                                                                               188-190 d                                     SMe           Me      OCF.sub.2 H                                              SEt           H       Me                                                       SEt           Me      Me                                                       SEt           H       OMe                                                      SEt           Me      OMe                                                      SEt           H       OCF.sub.2 H                                              SEt           Me      OCF.sub.2 H                                              S-- -n-Pr     H       Me         119-121                                       S-- -n-Pr     Me      Me                                                       S-- -n-Pr     H       OMe        140-145                                       S-- -n-Pr     Me      OMe                                                      S-- -n-Pr     H       OCF.sub.2 H                                              S-- -n-Pr     Me      OCF.sub.2 H                                              S-- .sub.-i-Pr                                                                               H       Me                                                       S-- .sub.-i-Pr                                                                               Me      Me                                                       S-- .sub.-i-Pr                                                                               H       OMe                                                      S-- .sub.-i-Pr                                                                               Me      OMe                                                      S-- .sub.-i-Pr                                                                               H       OCF.sub.2 H                                              S-- .sub.-i-Pr                                                                               Me      OCF.sub.2 H                                              O--allyl      H       Me                                                       O--allyl      Me      Me                                                       O--allyl      H       OMe                                                      O--allyl      Me      OMe                                                      O--allyl      H       OCF.sub.2 H                                              O--allyl      Me      OCF.sub.2 H                                              O--propargyl  H       Me                                                       O--propargyl  Me      Me                                                       O--propargyl  H       OMe                                                      O--propargyl  Me      OMe                                                      O--propargyl  H       OCF.sub.2 H                                              O--propargyl  Me      OCF.sub.2 H                                              CH.sub.2 F    H       Me                                                       CH.sub.2 F    Me      Me                                                       CH.sub.2 F    H       OMe                                                      CH.sub.2 F    Me      OMe                                                      CH.sub.2 F    H       OCF.sub.2 H                                              CH.sub.2 F    Me      OCF.sub.2 H                                              CHF.sub.2     H       Me                                                       CHF.sub.2     Me      Me                                                       CHF.sub.2     H       OMe                                                      CHF.sub.2     Me      OMe                                                      CHF.sub.2     H       OCF.sub.2 H                                              CHF.sub.2     Me      OCF.sub.2 H                                              CF.sub.3      H       Me         181-184 d                                     CF.sub.3      Me      Me                                                       CF.sub.3      H       OMe        165-167                                       CF.sub.3      Me      OMe                                                      CF.sub.3      H       OCF.sub.2 H                                                                               168-170                                       CF.sub.3      Me      OCF.sub.2 H                                              CH.sub.2 Cl   H       Me                                                       CH.sub.2 Cl   Me      Me                                                       CH.sub.2 Cl   H       OMe                                                      CH.sub.2 Cl   Me      OMe                                                      CH.sub.2 Cl   H       OCF.sub.2 H                                              CH.sub.2 Cl   Me      OCF.sub.2 H                                              CHCl.sub.2    H       Me                                                       CHCl.sub.2    Me      Me                                                       CHCl.sub.2    H       OMe                                                      CHCl.sub.2    Me      OMe                                                      CHCl.sub.2    H       OCF.sub.2 H                                              CHCl.sub.2    Me      OCF.sub.2 H                                              CCl.sub.3     H       Me                                                       CCl.sub.3     Me      Me                                                       CCl.sub.3     H       OMe                                                      CCl.sub.3     Me      OMe                                                      CCl.sub.3     H       OCF.sub.2 H                                              CCl.sub.3     Me      OCF.sub.2 H                                              CHFCH.sub.3   H       Me                                                       CHFCH.sub.3   Me      Me                                                       CHFCH.sub.3   H       OMe                                                      CHFCH.sub.3   Me      OMe                                                      CHFCH.sub.3   H       OCF.sub.2 H                                              CHFCH.sub.3   Me      OCF.sub.2 H                                              CF.sub.2 CH.sub.3                                                                            H       Me                                                       CF.sub.2 CH.sub.3                                                                            Me      Me                                                       CF.sub.2 CH.sub.3                                                                            H       OMe                                                      CF.sub.2 CH.sub.3                                                                            Me      OMe                                                      CF.sub.2 CH.sub.3                                                                            H       OCF.sub.2 H                                              CF.sub.2 CH.sub.3                                                                            Me      OCF.sub.2 H                                              CH.sub.2 CH.sub.2 F                                                                          H       Me                                                       CH.sub.2 CH.sub.2 F                                                                          Me      Me                                                       CH.sub.2 CH.sub.2 F                                                                          H       OMe                                                      CH.sub.2 CH.sub.2 F                                                                          Me      OMe                                                      CH.sub.2 CH.sub.2 F                                                                          H       OCF.sub.2 H                                              CH.sub.2 CH.sub.2 F                                                                          Me      OCF.sub.2 H                                              CH.sub.2 CHF.sub.2                                                                           H       Me                                                       CH.sub.2 CHF.sub.2                                                                           Me      Me                                                       CH.sub.2 CHF.sub.2                                                                           H       OMe                                                      CH.sub.2 CHF.sub.2                                                                           Me      OMe                                                      CH.sub.2 CHF.sub.2                                                                           H       OCF.sub.2 H                                              CH.sub.2 CHF.sub.2                                                                           Me      OCF.sub.2 H                                              CH.sub.2 CF.sub.3                                                                            H       Me                                                       CH.sub.2 CF.sub.3                                                                            Me      Me                                                       CH.sub.2 CF.sub.3                                                                            H       OMe                                                      CH.sub.2 CF.sub.3                                                                            Me      OMe                                                      CH.sub.2 CF.sub.3                                                                            H       OCF.sub.2 H                                              CH.sub.2 CF.sub.3                                                                            Me      OCF.sub.2 H                                              CHClCH.sub.3  H       Me                                                       CHClCH.sub.3  Me      Me                                                       CHClCH.sub.3  H       OMe                                                      CHClCH.sub.3  Me      OMe                                                      CHClCH.sub.3  H       OCF.sub.2 H                                              CHClCH.sub.3  Me      OCF.sub.2 H                                              CH.sub.2 OCH.sub.3                                                                           H       Me                                                       CH.sub.2 OCH.sub.3                                                                           Me      Me                                                       CH.sub.2 OCH.sub.3                                                                           H       OMe                                                      CH.sub.2 OCH.sub.3                                                                           Me      OMe                                                      CH.sub.2 OCH.sub.3                                                                           H       OCF.sub.2 H                                              CH.sub.2 OCH.sub.3                                                                           Me      OCF.sub.2 H                                              (CH.sub.2).sub.2 OCH.sub.3                                                                   H       Me                                                       (CH.sub. 2).sub.2 OCH.sub.3                                                                  Me      Me                                                       (CH.sub.2).sub.2 OCH.sub.3                                                                   H       OMe                                                      (CH.sub.2).sub.2 OCH.sub.3                                                                   Me      OMe                                                      (CH.sub.2).sub.2 OCH.sub.3                                                                   H       OCF.sub.2 H                                              (CH.sub.2).sub.2 OCH.sub.3                                                                   Me      OCF.sub.2 H                                              CH(OCH.sub.3)CH.sub.3                                                                        H       Me                                                       CH(OCH.sub.3)CH.sub.3                                                                        Me      Me                                                       CH(OCH.sub.3)CH.sub.3                                                                        H       OMe                                                      CH(OCH.sub.3)CH.sub.3                                                                        Me      OMe                                                      CH(OCH.sub.3)CH.sub.3                                                                        H       OCF.sub.2 H                                              CH(OCH.sub.3)CH.sub.3                                                                        Me      OCF.sub.2 H                                              CH.sub.2 SCH.sub.3                                                                           H       Me                                                       CH.sub.2 SCH.sub.3                                                                           Me      Me                                                       CH.sub.2 SCH.sub.3                                                                           H       OMe                                                      CH.sub.2 SCH.sub.3                                                                           Me      OMe                                                      CH.sub.2 SCH.sub.3                                                                           H       OCF.sub.2 H                                              CH.sub.2 SCH.sub.3                                                                           Me      OCF.sub.2 H                                              (CH.sub.2).sub.2 SCH.sub.3                                                                   H       Me                                                       (CH.sub.2).sub.2 SCH.sub.3                                                                   Me      Me                                                       (CH.sub.2).sub.2 SCH.sub.3                                                                   H       OMe                                                      (CH.sub.2).sub.2 SCH.sub.3                                                                   Me      OMe                                                      (CH.sub.2).sub.2 SCH.sub.3                                                                   H       OCF.sub.2 H                                              (CH.sub.2).sub.2 SCH.sub.3                                                                   Me      OCF.sub.2 H                                              CH(SCH.sub.3)CH.sub.3                                                                        H       Me                                                       CH(SCH.sub.3)CH.sub.3                                                                        Me      Me                                                       CH(SCH.sub.3)CH.sub.3                                                                        H       OMe                                                      CH(SCH.sub.3)CH.sub.3                                                                        Me      OMe                                                      CH(SCH.sub. 3)CH.sub.3                                                                       H       OCF.sub.2 H                                              CH(SCH.sub.3)CH.sub.3                                                                        Me      OCF.sub.2 H                                              OCF.sub.2 H   H       Me                                                       OCF.sub.2 H   Me      Me                                                       OCF.sub.2 H   H       OMe                                                      OCF.sub.2 H   Me      OMe                                                      OCF.sub.2 H   H       OCF.sub.2 H                                              OCF.sub.2 H   Me      OCF.sub.2 H                                              OCH.sub.2 CH.sub.2 F                                                                         H       Me                                                       OCH.sub.2 CH.sub.2 F                                                                         Me      Me                                                       OCH.sub.2 CH.sub.2 F                                                                         H       OMe                                                      OCH.sub.2 CH.sub.2 F                                                                         Me      OMe                                                      OCH.sub.2 CH.sub.2 F                                                                         H       OCF.sub.2 H                                              OCH.sub.2 CH.sub.2 F                                                                         Me      OCF.sub.2 H                                              OCH.sub.2 CHF.sub.2                                                                          H       Me                                                       OCH.sub.2 CHF.sub.2                                                                          Me      Me                                                       OCH.sub.2 CHF.sub.2                                                                          H       OMe                                                      OCH.sub.2 CHF.sub.2                                                                          Me      OMe                                                      OCH.sub.2 CHF.sub.2                                                                          H       OCF.sub.2 H                                              OCH.sub.2 CHF.sub.2                                                                          Me      OCF.sub.2 H                                              OCH.sub.2 CF.sub.3                                                                           H       Me                                                       OCH.sub.2 CF.sub.3                                                                           Me      Me                                                       OCH.sub.2 CF.sub.3                                                                           H       OMe                                                      OCH.sub.2 CF.sub.3                                                                           Me      OMe                                                      OCH.sub.2 CF.sub.3                                                                           H       OCF.sub.2 H                                              OCH.sub.2 CF.sub.3                                                                           Me      OCF.sub.2 H                                              O(CH.sub.2).sub.2 Cl                                                                         H       Me                                                       O(CH.sub.2).sub.2 Cl                                                                         Me      Me                                                       O(CH.sub.2).sub. 2 Cl                                                                        H       OMe                                                      O(CH.sub.2).sub.2 Cl                                                                         Me      OMe                                                      O(CH.sub.2).sub.2 Cl                                                                         H       OCF.sub.2 H                                              O(CH.sub.2).sub.2 Cl                                                                         Me      OCF.sub.2 H                                              S(O)Me        H       Me                                                       S(O)Me        Me      Me                                                       S(O)Me        H       OMe                                                      S(O)Me        Me      OMe                                                      S(O)Me        H       OCF.sub.2 H                                              S(O)Me        Me      OCF.sub.2 H                                              S(O)Et        H       Me                                                       S(O)Et        Me      Me                                                       S(O)Et        H       OMe                                                      S(O)Et        Me      OMe                                                      S(O)Et        H       OCF.sub.2 H                                              S(O)Et        Me      OCF.sub.2 H                                              S(O)-- -n-Pr  H       Me                                                       S(O)-- -n-Pr  Me      Me                                                       S(O)-- -n-Pr  H       OMe                                                      S(O)-- -n-Pr  Me      OMe                                                      S(O)-- -n-Pr  H       OCF.sub.2 H                                              S(O)-- -n-Pr  Me      OCF.sub.2 H                                              S(O)-- .sub.-i-Pr                                                                            H       Me                                                       S(O)-- .sub.-i-Pr                                                                            Me      Me                                                       S(O)-- .sub.-i-Pr                                                                            H       OMe                                                      S(O)-- .sub.-i-Pr                                                                            Me      Me                                                       S(O)-- .sub.-i-Pr                                                                            H       OCF.sub.2 H                                              S(O)-- .sub.-i-Pr                                                                            Me      OCF.sub.2 H                                              SO.sub.2 Me   H       Me                                                       SO.sub.2 Me   Me      Me                                                       SO.sub.2 Me   H       OMe                                                      SO.sub.2 Me   Me      OMe                                                      SO.sub.2 Me   H       OCF.sub.2 H                                              SO.sub.2 Me   Me      OCF.sub.2 H                                              SO.sub.2 Et   H       Me                                                       SO.sub.2 Et   Me      Me                                                       SO.sub.2 Et   H       OMe                                                      SO.sub.2 Et   Me      OMe                                                      SO.sub.2 Et   H       OCF.sub.2 H                                              SO.sub.2 Et   Me      OCF.sub.2 H                                              SO.sub.2 -- -n-Pr                                                                            H       Me                                                       SO.sub.2 -- -n-Pr                                                                            Me      Me                                                       SO.sub.2 -- -n-Pr                                                                            H       OMe                                                      SO.sub.2 -- -n-Pr                                                                            Me      OMe                                                      SO.sub.2 -- -n-Pr                                                                            H       OCF.sub.2 H                                              SO.sub.2 -- -n-Pr                                                                            Me      OCF.sub.2 H                                              SO.sub.2 -- .sub.-i-Pr                                                                       H       Me                                                       SO.sub.2 -- .sub.-i-Pr                                                                       Me      Me                                                       SO.sub.2 -- .sub.-i-Pr                                                                       H       OMe                                                      SO.sub.2 -- .sub.-i-Pr                                                                       Me      OMe                                                      SO.sub.2 -- .sub.-i-Pr                                                                       H       OCF.sub.2 H                                              SO.sub.2 -- .sub.-i-Pr                                                                       Me      OCF.sub.2 H                                              S--allyl      H       Me                                                       S--allyl      Me      Me                                                       S--allyl      H       OMe                                                      S--allyl      Me      OMe                                                      S--allyl      H       OCF.sub.2 H                                              S--allyl      Me      OCF.sub.2 H                                              S(O)allyl     H       Me                                                       S(O)allyl     Me      Me                                                       S(O)allyl     H       OMe                                                      S(O)allyl     Me      OMe                                                      S(O)allyl     H       OCF.sub.2 H                                              S(O)allyl     Me      OCF.sub.2 H                                              SO.sub.2 allyl                                                                               H       Me                                                       SO.sub.2 allyl                                                                               Me      Me                                                       SO.sub.2 allyl                                                                               H       OMe                                                      SO.sub.2 allyl                                                                               Me      OMe                                                      SO.sub.2 allyl                                                                               H       OCF.sub.2 H                                              SO.sub.2 allyl                                                                               Me      OCF.sub.2 H                                              S--propargyl  H       Me                                                       S--propargyl  Me      Me                                                       S--propargyl  H       OMe                                                      S--propargyl  Me      OMe                                                      S--propargyl  H       OCF.sub.2 H                                              S--propargyl  Me      OCF.sub.2 H                                              S(O)propargyl H       Me                                                       S(O)propargyl Me      Me                                                       S(O)propargyl H       OMe                                                      S(O)propargyl Me      OMe                                                      S(O)propargyl H       OCF.sub.2 H                                              S(O)propargyl Me      OCF.sub.2 H                                              SO.sub.2 propargyl                                                                           H       Me                                                       SO.sub.2 propargyl                                                                           Me      Me                                                       SO.sub.2 propargyl                                                                           H       OMe                                                      SO.sub.2 propargyl                                                                           Me      OMe                                                      SO.sub.2 propargyl                                                                           H       OCF.sub.2 H                                              SO.sub.2 propargyl                                                                           Me      OCF.sub.2 H                                              ______________________________________                                    

                  TABLE Ia                                                         ______________________________________                                         R.sub.1 = CH.sub.3                                                             R.sub.2         R       Y         m.p. (°C.)                            ______________________________________                                         CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       Me                                                     CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OMe                                                    CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       Me                                                     (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OMe                                                    (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            CH.sub.3                                                                               Me                                                     CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       Me                                                     CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       Me                                                     CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       OMe                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       Me                                                     (CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       OMe                                                    CH.sub.2 OCF.sub.2 H                                                                           H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                  CH.sub.3                                                                               OMe                                                    CH.sub.2 OCH.sub.2 CHF.sub.2                                                                   H       Me                                                     CH.sub.2 OCH.sub.2 CH.sub.2 Br                                                                 H       OMe                                                    CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                 H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CH.sub.2 I                                                                  H       Me                                                     CH.sub.2 OCF.sub.3                                                                             H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       Me                                                     CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OMe                                                    (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            CH.sub.3                                                                               OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       Me                                                     (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                    CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                            CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       Me                                                     CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       Me                                                     CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OMe                                                    (CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       OCF.sub.2 H                                            CH.sub. 2 S(O).sub.2 CH.sub.2 CH.sub.3                                                         H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OMe                                                    CH(CH.sub.3)S(O).sub.2 CH.sub.3                                                                H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          CH.sub.3                                                                               Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                  H       OMe                                                    CH.sub.2 S(O).sub.2 CF.sub.2 H                                                                 H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 F                                                        H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CHF.sub.2                                                         H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 Br                                                       H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 I                                                        CH.sub.3                                                                               OMe                                                    CH.sub.2 S(O).sub.2 CF.sub.3                                                                   H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                H       OMe                                                    OCH.sub.2 OCH.sub.3                                                                            H       OCF.sub.2 H                                            OCH.sub.2 OCH.sub.3                                                                            H       Me                                                     OCH.sub.2 OCH.sub.3                                                                            H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           CH.sub.3                                                                               OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OMe                                                    OCH.sub.2 OCH.sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            H       Me                                                     CH.sub.2 SCF.sub.2 H                                                                           H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.2 F                                                                  H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CHF.sub.2                                                                   H       Me                                                     CH.sub.2 SCH.sub.2 CH.sub.2 Br                                                                 H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.2 Cl                                                                 H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CH.sub.2 I                                                                  CH.sub.3                                                                               Me                                                     CH.sub.2 SCF.sub.3                                                                             H       Me                                                     CH.sub.2 S(O)CH.sub.3                                                                          H       OMe                                                    CH.sub.2 S(O)CH.sub.3                                                                          H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.3                                                                          H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OMe                                                    (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       Me                                                     CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 CH.sub.3                                                                               OMe                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         H       OMe                                                    CH(CH.sub.3)S(O)CH.sub.3                                                                       H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       Me                                                     CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       OMe                                                    CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                       H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                         H       OMe                                                    CH.sub.2 S(O)CF.sub.2 H                                                                        H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CH.sub.2 F                                                               CH.sub.3                                                                               OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CHF.sub.2                                                                H       Me                                                     CH.sub.2 S(O)CH.sub.2 CH.sub.2 Br                                                              H       OMe                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.2 I                                                               H       OCF.sub.2 H                                            CH.sub.2 S(O)CF.sub.3                                                                          H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OMe                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            OCH.sub.2 OCH.sub.2 CF.sub. 3                                                                  H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                           H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                         H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                         H       Me                                                     O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                         H       OMe                                                    O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                          H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCF.sub.3                                                                    H       Me                                                     OCH.sub.2 SCH.sub.3                                                                            H       OMe                                                    OCH.sub.2 SCH.sub.3                                                                            H       OCF.sub.2 H                                            OCH.sub.2 SCH.sub.3                                                                            H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OMe                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.3                                                                    CH.sub.3                                                                               Me                                                     O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OMe                                                    O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       Me                                                     OCH.sub.2 SCH.sub.2 CH.sub.3                                                                   H       OMe                                                    OCH.sub.2 SCH.sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                           H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(CH.sub. 2).sub.2 Cl                                                        H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                         CH.sub.3                                                                               OMe                                                    O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                          H       Me                                                     O(CH.sub.2).sub.2 SCF.sub.3                                                                    H       OMe                                                    OCH.sub.2 S(O)CH.sub.3                                                                         H       OCF.sub.2 H                                            OCH.sub.2 S(O)CH.sub.3                                                                         H       Me                                                     OCH.sub.2 S(O)CH.sub.3                                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                 H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                 H       Me                                                     O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                 H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        CH.sub.3                                                                               OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        H       Me                                                     OCH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                        H       OCF.sub.2 H                                            OCH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                H       Me                                                     O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                      H       OMe                                                    O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Cl                                                      H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Br                                                      H       Me                                                     O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 I                                                       H       OMe                                                    O(CH.sub.2).sub.2 S(O)CF.sub.3                                                                 H       OCF.sub.2 H                                            OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       OMe                                                    OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 CH.sub.3                                                                               Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       OCF.sub.2 H                                            OCH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                         H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                 H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                               H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Cl                                               H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Br                                               H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 I                                                CH.sub. 3                                                                              OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CF.sub.3                                                          H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                               H       OMe                                                    OCH.sub.2 S(O).sub.2 CF.sub.3                                                                  H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 CN                                                                           H       Me                                                     O(CH.sub.2).sub.2 CN                                                                           H       OMe                                                    O(CH.sub.2).sub.2 CN                                                                           H       OCF.sub.2 H                                            OCH.sub.2 CN    H       Me                                                     OCH.sub.2 CN    H       OMe                                                    OCH.sub.2 CN    H       OCF.sub.2 H                                            OCH.sub.2 CN    CH.sub.3                                                                               OCF.sub.2 H                                            OCH(CH.sub.3)CN H       Me                                                     O(CH.sub.2).sub.2 NH.sub.2                                                                     H       OMe                                                    O(CH.sub.2).sub.2 NH.sub.2                                                                     H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 NH.sub.2                                                                     H       Me                                                     O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       OMe                                                    O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       Me                                                     O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       OMe                                                    O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       Me                                                     SCH.sub.2 OCH.sub.3                                                                            H       OMe                                                    SCH.sub.2 OCH.sub.3                                                                            H       OCF.sub.2 H                                            SCH.sub.2 OCH.sub.3                                                                            H       Me                                                     SCH.sub.2 OCH.sub.2 CH.sub.3                                                                   H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCH.sub.3                                                                    CH.sub.3                                                                               Me                                                     S(CH.sub.2).sub.2 OCH.sub.3                                                                    H       Me                                                     S(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                           H       Me                                                     SCH.sub.2 OCH.sub.2 CF.sub.3                                                                   H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                         H       Me                                                     S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                         H       OMe                                                    S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                          H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCF.sub.3                                                                    CH.sub.3                                                                               OMe                                                    SCH.sub.2 SCH.sub.3                                                                            H       Me                                                     SCH.sub.2 SCH.sub.3                                                                            H       OMe                                                    SCH.sub.2 SCH.sub.3                                                                            H       OCF.sub.2 H                                            SCH.sub.2 SCH.sub.2 CH.sub.3                                                                   H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OMe                                                    S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OMe                                                    SCH(CH.sub.3)SCH.sub.3                                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                           CH.sub.3                                                                               OCF.sub.2 H                                            SCH.sub.2 SCH.sub.2 CF.sub.3                                                                   H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                         H       OMe                                                    S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                         H       Me                                                     S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                          H       OMe                                                    S(CH.sub.2).sub.2 SCF.sub.3                                                                    H       OCF.sub.2 H                                            SCH.sub.2 CN    H       Me                                                     SCH.sub.2 CN    H       OMe                                                    SCH.sub.2 CN    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CN                                                                           H       Me                                                     S(CH.sub.2).sub.2 CN                                                                           H       OMe                                                    S(CH.sub.2).sub.2 CN                                                                           H       OCF.sub.2 H                                            SCH(CH.sub.3)CN H       Me                                                     SCHF.sub.2      H       OMe                                                    SCHF.sub.2      H       OCF.sub.2 H                                            SCHF.sub.2      CH.sub.3                                                                               Me                                                     SCHF.sub.2      H       Me                                                     SCF.sub.3       H       OMe                                                    SCH.sub.2 CFH.sub.2                                                                            H       OCF.sub.2 H                                            SCH.sub.2 CF.sub.2 H                                                                           H       Me                                                     SCH.sub.2 CF.sub.3                                                                             H       OMe                                                    SCH.sub.2 CF.sub.3                                                                             H       OCF.sub.2 H                                            SCH.sub.2 CF.sub.3                                                                             H       Me                                                     SCH.sub.2 CF.sub.2 H                                                                           H       OMe                                                    S(CH.sub.2).sub.2 CFH.sub.2                                                                    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CClH.sub.2                                                                   CH.sub.3                                                                               OMe                                                    S(CH.sub.2).sub.2 CIH.sub.2                                                                    H       Me                                                     SCF.sub.2 CF.sub.3                                                                             H       OMe                                                    SCH(CH.sub.3)CF.sub.3                                                                          H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CCl.sub.3                                                                    H       Me                                                     S(O)CHF.sub.2   H       OMe                                                    S(O)CHF.sub.2   H       OCF.sub.2 H                                            S(O)CHF.sub.2   H       Me                                                     S(O)CF.sub.3    H       OMe                                                    S(O)CH.sub.2 CFH.sub.2                                                                         H       OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.2 H                                                                        CH.sub.3                                                                               OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.3                                                                          H       Me                                                     S(O)CH.sub.2 CF.sub.3                                                                          H       OMe                                                    S(O)CH.sub.2 CF.sub.3                                                                          H       OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.2 H                                                                        H       Me                                                     S(O)(CH.sub.2).sub.2 CFH.sub.2                                                                 H       OMe                                                    S(O)(CH.sub.2).sub.2 CClH.sub.2                                                                H       OCF.sub.2 H                                            S(O)(CH.sub.2).sub.2 CIH.sub.2                                                                 H       Me                                                     S(O)CF.sub.2 CF.sub.3                                                                          H       OMe                                                    S(O)CH(CH.sub.3)CF.sub.3                                                                       H       OCF.sub.2 H                                            S(O)(CH.sub.2).sub.2 CCl.sub.3                                                                 H       Me                                                     S(O).sub.2 CHF.sub.2                                                                           H       OMe                                                    S(O).sub.2 CHF.sub.2                                                                           H       OCF.sub.2 H                                            S(O).sub.2 CHF.sub.2                                                                           H       Me                                                     S(O).sub.2 CF.sub.3                                                                            H       OMe                                                    S(O).sub.2 CH.sub.2 CFH.sub.2                                                                  H       OCF.sub.2 H                                            S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                 CH.sub.3                                                                               Me                                                     S(O).sub.2 CH.sub.2 CF.sub.3                                                                   H       Me                                                     S(O).sub.2 CH.sub.2 CF.sub.3                                                                   H       OMe                                                    S(O).sub. 2 CH.sub.2 CF.sub.3                                                                  H       OCF.sub.2 H                                            S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                 H       Me                                                     S(O).sub.2 (CH.sub.2).sub.2 CFH.sub.2                                                          H       OMe                                                    S(O).sub.2 (CH.sub.2).sub.2 CClH.sub.2                                                         H       OCF.sub.2 H                                            S(O).sub.2 (CH.sub.2).sub.2 CIH.sub.2                                                          H       Me                                                     S(O).sub.2 CF.sub.2 CF.sub.3                                                                   H       OMe                                                    S(O).sub.2 CH(CH.sub.3)CF.sub.3                                                                H       OCF.sub.2 H                                            S(O).sub.2 (CH.sub.2).sub.2 CCl.sub.3                                                          CH.sub.3                                                                               OMe                                                    S(O).sub.2 CH.sub.2 Cl                                                                         H       Me                                                     CH═CH.sub.2 H       OMe                                                    CH═CH.sub.2 H       OCF.sub.2 H                                            CH═CH.sub.2 H       Me                                                     CH.sub.2 CH═CH.sub.2                                                                       H       OMe                                                    CH.sub.2 CH═CH.sub.2                                                                       H       OCF.sub.2 H                                            CH.sub.2 CH═CH.sub.2                                                                       H       Me                                                     CH═CHCH.sub.3                                                                              H       OMe                                                    C(CH.sub.3)═CH.sub.2                                                                       H       OCF.sub.2 H                                            CH═CH.sub.2 CH.sub.3                                                                               OCF.sub.2 H                                            C.tbd.CH        H       Me                                                     C.tbd.CH        H       OMe                                                    C.tbd.CH        H       OCF.sub.2 H                                            CH.sub.2 C.tbd.CH                                                                              H       Me                                                     CH.sub.2 C.tbd.CH                                                                              H       OMe                                                    CH.sub.2 C.tbd.CH                                                                              H       OCF.sub.2 H                                            C.tbd.CCH.sub.3 H       Me                                                     C.tbd.CCH.sub.3 H       OMe                                                    C.tbd.CCH.sub.3 H       OCF.sub.2 H                                            NH.sub. 2       H       Me                                                     NH.sub.2        H       OMe                                                    NH.sub.2        H       OCF.sub.2 H                                            NHCH.sub.3      H       Me                                                     NHCH.sub.3      H       OMe                                                    NHCH.sub.3      H       OCF.sub.2 H                                            NHCH.sub.3      CH.sub.3                                                                               Me                                                     N(CH.sub.3).sub.2                                                                              H       Me                                                     N(CH.sub.3)2    H       OMe                                                    N(CH.sub.3).sub.2                                                                              H       OCF.sub.2 H                                            NHCH.sub.2 CH.sub.3                                                                            H       Me                                                     NHCH.sub.2 CH.sub.3                                                                            H       OMe                                                    NHCH.sub.2 CH.sub.3                                                                            H       OCF.sub.2 H                                            N(CH.sub.3)CH.sub.2 CH.sub.3                                                                   H       Me                                                     N(CH.sub.2 CH.sub.3).sub.2                                                                     H       OMe                                                    NHCH.sub.2 CF.sub.3                                                                            H       OCF.sub.2 H                                            NHCH.sub.2 CF.sub.3                                                                            CH.sub.3                                                                               OMe                                                    NHCH.sub.2 CF.sub.3                                                                            H       Me                                                     NHCH.sub.2 CF.sub.3                                                                            H       OMe                                                    N(CH.sub.3)CH.sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                            N(CH.sub.3)CH.sub.2 CHF.sub.2                                                                  H       Me                                                     N(CH.sub.3)(CH.sub.2).sub.2 F                                                                  H       OMe                                                    N(CH.sub.3)(CH.sub.2).sub.2 Cl                                                                 H       OCF.sub.2 H                                            N(CH.sub.3)(CH.sub.2).sub.2 I                                                                  H       Me                                                     N(CH.sub.3)(CH.sub.2).sub.2 Br                                                                 H       OMe                                                    NHCF.sub.3      CH.sub.3                                                                               OCF.sub.2 H                                            NHCF.sub.3      H       Me                                                     NH(CH.sub.2).sub.2 F                                                                           H       OMe                                                    N(CH.sub.3)CF.sub.2 H                                                                          H       OCF.sub.2 H                                            NHCF.sub.2 H    H       Me                                                     ______________________________________                                    

                  TABLE II                                                         ______________________________________                                         R.sub.1 = Et                                                                   R.sub.2       R       Y          m.p. (°C.)                             ______________________________________                                         Me            H       Me         --                                            Me            Me      Me                                                       Me            H       OMe        121-133 d                                     Me            Me      OMe                                                      Me            H       OCF.sub.2 H                                                                               163-165 d                                     Me            Me      OCF.sub.2 H                                              Et            H       Me                                                       Et            Me      Me                                                       Et            H       OMe                                                      Et            Me      OMe                                                      Et            H       OCF.sub.2 H                                              Et            Me      OCF.sub.2 H                                               -n-Pr        H       Me                                                        -n-Pr        Me      Me                                                        -n-Pr        H       OMe                                                       -n-Pr        Me      OMe                                                       -n-Pr        H       OCF.sub.2 H                                               -n-Pr        Me      OCF.sub.2 H                                               .sub.-i-Pr   H       Me                                                        .sub.-i-Pr   Me      Me                                                        .sub.-i-Pr   H       OMe                                                       .sub.-i-Pr   Me      OMe                                                       .sub.-i-Pr   H       OCF.sub.2 H                                               .sub.-i-Pr   Me      OCF.sub.2 H                                              cyclo-Pr      H       Me                                                       cyclo-Pr      Me      Me                                                       cyclo-Pr      H       OMe                                                      cyclo-Pr      Me      OMe                                                      cyclo-Pr      H       OCF.sub.2 H                                              cyclo-Pr      Me      OCF.sub.2 H                                              OMe           H       Me         172-178 d                                     OMe           Me      Me                                                       OMe           H       OMe        180-184 d                                     OMe           Me      OMe                                                      OMe           H       OCF.sub.2 H                                                                               162-166                                       OMe           Me      OCF.sub.2 H                                              OEt           H       Me                                                       OEt           Me      Me                                                       OEt           H       OMe                                                      OEt           Me      OMe                                                      OEt           H       OCF.sub.2 H                                              OEt           Me      OCF.sub.2 H                                              O-- -n-Pr     H       Me                                                       O-- -n-Pr     Me      Me                                                       O-- -n-Pr     H       OMe                                                      O-- -n-Pr     Me      OMe                                                      O-- -n-Pr     H       OCF.sub.2 H                                              O-- -n-Pr     Me      OCF.sub.2 H                                              O-- .sub.-i-Pr                                                                               H       Me         164-168                                       O-- .sub.-i-Pr                                                                               Me      Me                                                       O-- .sub.-i-Pr                                                                               H       OMe        147-150                                       O-- .sub.-i-Pr                                                                               Me      OMe                                                      O-- .sub.-i-Pr                                                                               H       OCF.sub.2 H                                              O-- .sub.-i-Pr                                                                               Me      OCF.sub.2 H                                              SMe           H       Me         151-155                                       SMe           Me      Me                                                       SMe           H       OMe        149-154                                       SMe           Me      OMe                                                      SMe           H       OCF.sub.2 H                                              SMe           Me      OCF.sub.2 H                                              SEt           H       Me         134-139                                       SEt           Me      Me                                                       SEt           H       OMe        121-126                                       SEt           Me      OMe                                                      SEt           H       OCF.sub.2 H                                              SEt           Me      OCF.sub.2 H                                              S-- -n-Pr     H       Me                                                       S-- -n-Pr     Me      Me                                                       S-- -n-Pr     H       OMe        130-134                                       S-- -n-Pr     Me      OMe                                                      S-- -n-Pr     H       OCF.sub.2 H                                              S-- -n-Pr     Me      OCF.sub.2 H                                              S-- .sub.-i-Pr                                                                               H       Me         135-140                                       S-- .sub.-i-Pr                                                                               Me      Me                                                       S-- .sub.-i-Pr                                                                               H       OMe        145-150                                       S-- .sub.-i-Pr                                                                               Me      OMe                                                      S-- .sub.-i-Pr                                                                               H       OCF.sub.2 H                                              S-- .sub.-i-Pr                                                                               Me      OCF.sub.2 H                                              O--allyl      H       Me                                                       O--allyl      Me      Me                                                       O--allyl      H       OMe                                                      O--allyl      Me      OMe                                                      O--allyl      H       OCF.sub.2 H                                              O--allyl      Me      OCF.sub.2 H                                              O--propargyl  H       Me                                                       O--propargyl  Me      Me                                                       O--propargyl  H       OMe                                                      O--propargyl  Me      OMe                                                      O--propargyl  H       OCF.sub.2 H                                              O--propargyl  Me      OCF.sub.2 H                                              CH.sub.2 F    H       Me                                                       CH.sub.2 F    Me      Me                                                       CH.sub.2 F    H       OMe                                                      CH.sub.2 F    Me      OMe                                                      CH.sub.2 F    H       OCF.sub.2 H                                              CH.sub.2 F    Me      OCF.sub.2 H                                              CHF.sub.2     H       Me                                                       CHF.sub.2     Me      Me                                                       CHF.sub.2     H       OMe                                                      CHF.sub.2     Me      OMe                                                      CHF.sub.2     H       OCF.sub.2 H                                              CHF.sub.2     Me      OCF.sub.2 H                                              CF.sub.3      H       Me         173-175                                       CF.sub.3      Me      Me                                                       CF.sub.3      H       OMe        115-120                                       CF.sub.3      Me      OMe                                                      CF.sub.3      H       OCF.sub.2 H                                              CF.sub.3      Me      OCF.sub.2 H                                              CH.sub.2 Cl   H       Me                                                       CH.sub.2 Cl   Me      Me                                                       CH.sub.2 Cl   H       OMe                                                      CH.sub.2 Cl   Me      OMe                                                      CH.sub.2 Cl   H       OCF.sub.2 H                                              CH.sub.2 Cl   Me      OCF.sub.2 H                                              CHCl.sub.2    H       Me                                                       CHCl.sub.2    Me      Me                                                       CHCl.sub.2    H       OMe                                                      CHCl.sub.2    Me      OMe                                                      CHCl.sub.2    H       OCF.sub.2 H                                              CHCl.sub.2    Me      OCF.sub.2 H                                              CCl.sub.3     H       Me                                                       CCl.sub.3     Me      Me                                                       CCl.sub.3     H       OMe                                                      CCl.sub.3     Me      OMe                                                      CCl.sub.3     H       OCF.sub.2 H                                              CCl.sub.3     Me      OCF.sub.2 H                                              CHFCH.sub.3   H       Me                                                       CHFCH.sub.3   Me      Me                                                       CHFCH.sub.3   H       OMe                                                      CHFCH.sub.3   Me      OMe                                                      CHFCH.sub.3   H       OCF.sub.2 H                                              CHFCH.sub.3   Me      OCF.sub.2 H                                              CF.sub.2 CH.sub.3                                                                            H       Me                                                       CF.sub.2 CH.sub.3                                                                            Me      Me                                                       CF.sub.2 CH.sub.3                                                                            H       OMe                                                      CF.sub.2 CH.sub.3                                                                            Me      OMe                                                      CF.sub.2 CH.sub.3                                                                            H       OCF.sub.2 H                                              CF.sub.2 CH.sub.3                                                                            Me      OCF.sub.2 H                                              CH.sub.2 CH.sub.2 F                                                                          H       Me                                                       CH.sub.2 CH.sub.2 F                                                                          Me      Me                                                       CH.sub.2 CH.sub.2 F                                                                          H       OMe                                                      CH.sub.2 CH.sub.2 F                                                                          Me      OMe                                                      CH.sub.2 CH.sub.2 F                                                                          H       OCF.sub.2 H                                              CH.sub.2 CH.sub.2 F                                                                          Me      OCF.sub.2 H                                              CH.sub.2 CHF.sub.2                                                                           H       Me                                                       CH.sub.2 CHF.sub.2                                                                           Me      Me                                                       CH.sub.2 CHF.sub.2                                                                           H       OMe                                                      CH.sub.2 CHF.sub.2                                                                           Me      OMe                                                      CH.sub.2 CHF.sub.2                                                                           H       OCF.sub.2 H                                              CH.sub.2 CHF.sub.2                                                                           Me      OCF.sub.2 H                                              CH.sub.2 CF.sub.3                                                                            H       Me                                                       CH.sub.2 CF.sub.3                                                                            Me      Me                                                       CH.sub.2 CF.sub.3                                                                            H       OMe                                                      CH.sub.2 CF.sub.3                                                                            Me      OMe                                                      CH.sub.2 CF.sub.3                                                                            H       OCF.sub.2 H                                              CH.sub.2 CF.sub.3                                                                            Me      OCF.sub.2 H                                              CHClCH.sub.3  H       Me                                                       CHClCH.sub.3  Me      Me                                                       CHClCH.sub.3  H       OMe                                                      CHClCH.sub.3  Me      OMe                                                      CHClCH.sub.3  H       OCF.sub.2 H                                              CHClCH.sub.3  Me      OCF.sub.2 H                                              CH.sub.2 OCH.sub.3                                                                           H       Me                                                       CH.sub.2 OCH.sub.3                                                                           Me      Me                                                       CH.sub.2 OCH.sub.3                                                                           H       OMe                                                      CH.sub.2 OCH.sub.3                                                                           Me      OMe                                                      CH.sub.2 OCH.sub.3                                                                           H       OCF.sub.2 H                                              CH.sub.2 OCH.sub.3                                                                           Me      OCF.sub.2 H                                              (CH.sub.2).sub.2 OCH.sub.3                                                                   H       Me                                                       (CH.sub.2).sub.2 OCH.sub.3                                                                   Me      Me                                                       (CH.sub.2).sub.2 OCH.sub.3                                                                   H       OMe                                                      (CH.sub.2).sub.2 OCH.sub.3                                                                   Me      OMe                                                      (CH.sub.2).sub.2 OCH.sub.3                                                                   H       OCF.sub.2 H                                              (CH.sub.2).sub.2 OCH.sub.3                                                                   Me      OCF.sub.2 H                                              CH(OCH.sub.3)CH.sub.3                                                                        H       Me                                                       CH(OCH.sub.3)CH.sub.3                                                                        Me      Me                                                       CH(OCH.sub.3)CH.sub.3                                                                        H       OMe                                                      CH(OCH.sub.3)CH.sub.3                                                                        Me      OMe                                                      CH(OCH.sub.3)CH.sub.3                                                                        H       OCF.sub.2 H                                              CH(OCH.sub.3)CH.sub.3                                                                        Me      OCF.sub.2 H                                              CH.sub.2 SCH.sub.3                                                                           H       Me                                                       CH.sub.2 SCH.sub.3                                                                           Me      Me                                                       CH.sub.2 SCH.sub.3                                                                           H       OMe                                                      CH.sub.2 SCH.sub.3                                                                           Me      OMe                                                      CH.sub.2 SCH.sub.3                                                                           H       OCF.sub.2 H                                              CH.sub.2 SCH.sub.3                                                                           Me      OCF.sub.2 H                                              (CH.sub.2).sub.2 SCH.sub.3                                                                   H       Me                                                       (CH.sub.2).sub.2 SCH.sub.3                                                                   Me      Me                                                       (CH.sub.2).sub.2 SCH.sub.3                                                                   H       OMe                                                      (CH.sub.2).sub.2 SCH.sub.3                                                                   Me      OMe                                                      (CH.sub.2 ).sub.2 SCH.sub.3                                                                  H       OCF.sub.2 H                                              (CH.sub.2).sub.2 SCH.sub.3                                                                   Me      OCF.sub.2 H                                              CH(SCH.sub.3)CH.sub.3                                                                        H       Me                                                       CH(SCH.sub.3)CH.sub.3                                                                        Me      Me                                                       CH(SCH.sub.3)CH.sub.3                                                                        H       OMe                                                      CH(SCH.sub.3)CH.sub.3                                                                        Me      OMe                                                      CH(SCH.sub.3)CH.sub.3                                                                        H       OCF.sub.2 H                                              CH(SCH.sub.3)CH.sub.3                                                                        Me      OCF.sub.2 H                                              OCF.sub.2 H   H       Me                                                       OCF.sub.2 H   Me      Me                                                       OCF.sub.2 H   H       OMe                                                      OCF.sub.2 H   Me      OMe                                                      OCF.sub.2 H   H       OCF.sub.2 H                                              OCF.sub.2 H   Me      OCF.sub.2 H                                              OCH.sub.2 CH.sub.2 F                                                                         H       Me                                                       OCH.sub.2 CH.sub.2 F                                                                         Me      Me                                                       OCH.sub.2 CH.sub.2 F                                                                         H       OMe                                                      OCH.sub.2 CH.sub.2 F                                                                         Me      OMe                                                      OCH.sub.2 CH.sub.2 F                                                                         H       OCF.sub.2 H                                              OCH.sub.2 CH.sub.2 F                                                                         Me      OCF.sub.2 H                                              OCH.sub.2 CHF.sub.2                                                                          H       Me                                                       OCH.sub.2 CHF.sub.2                                                                          Me      Me                                                       OCH.sub.2 CHF.sub.2                                                                          H       OMe                                                      OCH.sub.2 CHF.sub.2                                                                          Me      OMe                                                      OCH.sub.2 CHF.sub.2                                                                          H       OCF.sub.2 H                                              OCH.sub.2 CHF.sub.2                                                                          Me      OCF.sub.2 H                                              OCH.sub.2 CF.sub.3                                                                           H       Me                                                       OCH.sub.2 CF.sub.3                                                                           Me      Me                                                       OCH.sub.2 CF.sub.3                                                                           H       OMe                                                      OCH.sub.2 CF.sub.3                                                                           Me      OMe                                                      OCH.sub.2 CF.sub.3                                                                           H       OCF.sub.2 H                                              OCH.sub.2 CF.sub.3                                                                           Me      OCF.sub.2 H                                              O(CH.sub.2).sub.2 Cl                                                                         H       Me                                                       O(CH.sub.2).sub.2 Cl                                                                         Me      Me                                                       O(CH.sub.2).sub.2 Cl                                                                         H       OMe                                                      O(CH.sub.2).sub.2 Cl                                                                         Me      OMe                                                      O(CH.sub.2).sub.2 Cl                                                                         H       OCF.sub.2 H                                              O(CH.sub.2).sub.2 Cl                                                                         Me      OCF.sub.2 H                                              S(O)Me        H       Me                                                       S(O)Me        Me      Me                                                       S(O)Me        H       OMe                                                      S(O)Me        Me      OMe                                                      S(O)Me        H       OCF.sub.2 H                                              S(O)Me        Me      OCF.sub.2 H                                              S(O)Et        H       Me                                                       S(O)Et        Me      Me                                                       S(O)Et        H       OMe                                                      S(O)Et        Me      OMe                                                      S(O)Et        H       OCF.sub.2 H                                              S(O)Et        Me      OCF.sub.2 H                                              S(O)-- -n-Pr  H       Me         105-110                                       S(O)-- -n-Pr  Me      Me                                                       S(O)-- -n-Pr  H       OMe        85-91                                         S(O)-- -n-Pr  Me      OMe                                                      S(O)-- -n-Pr  H       OCF.sub.2 H                                              S(O)-- -n-Pr  Me      OCF.sub.2 H                                              S(O)-- .sub.-i-Pr                                                                            H       Me                                                       S(O)-- .sub.-i-Pr                                                                            Me      Me                                                       S(O)-- .sub.-i-Pr                                                                            H       OMe                                                      S(O)-- .sub.-i-Pr                                                                            Me      Me                                                       S(O)-- .sub.-i-Pr                                                                            H       OCF.sub.2 H                                              S(O)-- .sub.-i-Pr                                                                            Me      OCF.sub.2 H                                              SO.sub.2 Me   H       Me                                                       SO.sub.2 Me   Me      Me                                                       SO.sub.2 Me   H       OMe                                                      SO.sub.2 Me   Me      OMe                                                      SO.sub.2 Me   H       OCF.sub.2 H                                              SO.sub.2 Me   Me      OCF.sub.2 H                                              SO.sub.2 Et   H       Me                                                       SO.sub.2 Et   Me      Me                                                       SO.sub.2 Et   H       OMe                                                      SO.sub.2 Et   Me      OMe                                                      SO.sub.2 Et   H       OCF.sub.2 H                                              SO.sub.2 Et   Me      OCF.sub.2 H                                              SO.sub.2 -- -n-Pr                                                                            H       Me                                                       SO.sub.2 -- -n-Pr                                                                            Me      Me                                                       SO.sub.2 -- -n-Pr                                                                            H       OMe                                                      SO.sub.2 -- -n-Pr                                                                            Me      OMe                                                      SO.sub.2 -- -n-Pr                                                                            H       OCF.sub.2 H                                              SO.sub.2 -- -n-Pr                                                                            Me      OCF.sub.2 H                                              SO.sub.2 -- .sub.-i-Pr                                                                       H       Me                                                       SO.sub.2 -- .sub.-i-Pr                                                                       Me      Me                                                       SO.sub.2 -- .sub.-i-Pr                                                                       H       OMe                                                      SO.sub.2 -- .sub.-i-Pr                                                                       Me      OMe                                                      SO.sub.2 -- .sub.-i-Pr                                                                       H       OCF.sub.2 H                                              SO.sub.2 -- -i-Pr                                                                            Me      OCF.sub.2 H                                              S--allyl      H       Me                                                       S--allyl      Me      Me                                                       S--allyl      H       OMe                                                      S--allyl      Me      OMe                                                      S--allyl      H       OCF.sub.2 H                                              S--allyl      Me      OCF.sub.2 H                                              S(O)allyl     H       Me                                                       S(O)allyl     Me      Me                                                       S(O)allyl     H       OMe                                                      S(O)allyl     Me      OMe                                                      S(O)allyl     H       OCF.sub.2 H                                              S(O)allyl     Me      OCF.sub.2 H                                              SO.sub.2 allyl                                                                               H       Me                                                       SO.sub.2 allyl                                                                               Me      Me                                                       SO.sub.2 allyl                                                                               H       OMe                                                      SO.sub.2 allyl                                                                               Me      OMe                                                      SO.sub.2 allyl                                                                               H       OCF.sub.2 H                                              SO.sub.2 allyl                                                                               Me      OCF.sub.2 H                                              S--propargyl  H       Me                                                       S--propargyl  Me      Me                                                       S--propargyl  H       OMe                                                      S--propargyl  Me      OMe                                                      S--propargyl  H       OCF.sub.2 H                                              S--propargyl  Me      OCF.sub.2 H                                              S(O)propargyl H       Me                                                       S(O)propargyl Me      Me                                                       S(O)propargyl H       OMe                                                      S(O)propargyl Me      OMe                                                      S(O)propargyl H       OCF.sub.2 H                                              S(O)propargyl Me      OCF.sub.2 H                                              SO.sub.2 propargyl                                                                           H       Me                                                       SO.sub.2 propargyl                                                                           Me      Me                                                       SO.sub.2 propargyl                                                                           H       OMe                                                      SO.sub.2 propargyl                                                                           Me      OMe                                                      SO.sub.2 propargyl                                                                           H       OCF.sub.2 H                                              SO.sub.2 propargyl                                                                           Me      OCF.sub.2 H                                              ______________________________________                                    

                  TABLE IIa                                                        ______________________________________                                         R.sub.1 = Et                                                                   R.sub.2         R       Y         m.p. (°C.)                            ______________________________________                                         CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       Me                                                     CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OMe                                                    CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       Me                                                     (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OMe                                                    (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            CH.sub.3                                                                               Me                                                     CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       Me                                                     CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       Me                                                     CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       OMe                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       Me                                                     (CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       OMe                                                    CH.sub.2 OCF.sub.2 H                                                                           H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                  CH.sub.3                                                                               OMe                                                    CH.sub.2 OCH.sub.2 CHF.sub.2                                                                   H       Me                                                     CH.sub.2 OCH.sub.2 CH.sub. 2 Br                                                                H       OMe                                                    CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                 H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CH.sub.2 I                                                                  H       Me                                                     CH.sub.2 OCF.sub.3                                                                             H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       Me                                                     CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OMe                                                    (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            CH.sub.3                                                                               OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       Me                                                     (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                    CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                            CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       Me                                                     CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       Me                                                     CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OMe                                                    (CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OMe                                                    CH(CH.sub.3)S(O).sub.2 CH.sub.3                                                                H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          CH.sub.3                                                                               Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                  H       OMe                                                    CH.sub.2 S(O).sub.2 CF.sub.2 H                                                                 H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 F                                                        H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CHF.sub.2                                                         H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 Br                                                       H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 I                                                        CH.sub.3                                                                               OMe                                                    CH.sub.2 S(O).sub.2 CF.sub.3                                                                   H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                H       OMe                                                    OCH.sub.2 OCH.sub.3                                                                            H       OCF.sub.2 H                                            OCH.sub.2 OCH.sub.3                                                                            H       Me                                                     OCH.sub.2 OCH.sub.3                                                                            H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OCF.sub. 2 H                                           O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           CH.sub.3                                                                               OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OMe                                                    OCH.sub.2 OCH.sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            H       Me                                                     CH.sub.2 SCF.sub.2 H                                                                           H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.2 F                                                                  H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CHF.sub.2                                                                   H       Me                                                     CH.sub.2 SCH.sub.2 CH.sub.2 Br                                                                 H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.2 Cl                                                                 H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CH.sub.2 I                                                                  CH.sub.3                                                                               Me                                                     CH.sub.2 SCF.sub.3                                                                             H       Me                                                     CH.sub.2 S(O)CH.sub.3                                                                          H       OMe                                                    CH.sub.2 S(O)CH.sub.3                                                                          H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.3                                                                          H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OMe                                                    (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       Me                                                     CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH.sub. 2 S(O)CH.sub.2 CH.sub.3                                                                H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 CH.sub.3                                                                               OMe                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         H       OMe                                                    CH(CH.sub.3)S(O)CH.sub.3                                                                       H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       Me                                                     CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       OMe                                                    CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                       H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                         H       OMe                                                    CH.sub.2 S(O)CF.sub.2 H                                                                        H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CH.sub.2 F                                                               CH.sub.3                                                                               OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CHF.sub.2                                                                H       Me                                                     CH.sub.2 S(O)CH.sub.2 CH.sub.2 Br                                                              H       OMe                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.2 I                                                               H       OCF.sub.2 H                                            CH.sub.2 S(O)CF.sub.3                                                                          H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OMe                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            OCH.sub.2 OCH.sub.2 CF.sub.3                                                                   H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                           H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                         H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                         H       Me                                                     O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                         H       OMe                                                    O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                          H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCF.sub.3                                                                    H       Me                                                     OCH.sub.2 SCH.sub.3                                                                            H       OMe                                                    OCH.sub.2 SCH.sub.3                                                                            H       OCF.sub.2 H                                            OCH.sub.2 SCH.sub.3                                                                            H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OMe                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.3                                                                    CH.sub.3                                                                               Me                                                     O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OMe                                                    O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       Me                                                     OCH.sub.2 SCH.sub.2 CH.sub.3                                                                   H       OMe                                                    OCH.sub.2 SCH.sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                           H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(CH.sub.2 ).sub.2 Cl                                                        H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                         CH.sub.3                                                                               OMe                                                    O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                          H       Me                                                     O(CH.sub.2).sub.2 SCF.sub.3                                                                    H       OMe                                                    OCH.sub.2 S(O)CH.sub.3                                                                         H       OCF.sub.2 H                                            OCH.sub.2 S(O)CH.sub.3                                                                         H       Me                                                     OCH.sub.2 S(O)CH.sub.3                                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                 H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                 H       Me                                                     O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                 H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        CH.sub.3                                                                               OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        H       Me                                                     OCH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                        H       OCF.sub.2 H                                            OCH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                H       Me                                                     O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                      H       OMe                                                    O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Cl                                                      H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Br                                                      H       Me                                                     O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 I                                                       H       OMe                                                    O(CH.sub.2).sub.2 S(O)CF.sub.3                                                                 H       OCF.sub.2 H                                            OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       OMe                                                    OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 CH.sub.3                                                                               Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       OCF.sub.2 H                                            OCH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                         H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                 H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                               H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Cl                                               H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Br                                               H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 I                                                CH.sub.3                                                                               OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CF.sub.3                                                          H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                               H       OMe                                                    OCH.sub.2 S(O).sub.2 CF.sub.3                                                                  H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 CN                                                                           H       Me                                                     O(CH.sub.2).sub.2 CN                                                                           H       OMe                                                    O(CH.sub.2).sub.2 CN                                                                           H       OCF.sub.2 H                                            OCH.sub.2 CN    H       Me                                                     OCH.sub.2 CN    H       OMe                                                    OCH.sub.2 CN    H       OCF.sub.2 H                                            OCH.sub.2 CN    CH.sub.3                                                                               OCF.sub.2 H                                            OCH(CH.sub.3)CN H       Me                                                     O(CH.sub.2).sub.2 NH.sub.2                                                                     H       OMe                                                    O(CH.sub.2).sub.2 NH.sub.2                                                                     H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 NH.sub.2                                                                     H       Me                                                     O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       OMe                                                    O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       Me                                                     O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       OMe                                                    O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       Me                                                     SCH.sub.2 OCH.sub.3                                                                            H       OMe                                                    SCH.sub.2 OCH.sub.3                                                                            H       OCF.sub.2 H                                            SCH.sub.2 OCH.sub.3                                                                            H       Me                                                     SCH.sub.2 OCH.sub.2 CH.sub.3                                                                   H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub. 3                                                                   H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCH.sub.3                                                                    CH.sub.3                                                                               Me                                                     S(CH.sub.2).sub.2 OCH.sub.3                                                                    H       Me                                                     S(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                           H       Me                                                     SCH.sub.2 OCH.sub.2 CF.sub.3                                                                   H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                         H       Me                                                     S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                         H       OMe                                                    S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                          H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCF.sub.3                                                                    CH.sub.3                                                                               OMe                                                    SCH.sub.2 SCH.sub.3                                                                            H       Me                                                     SCH.sub.2 SCH.sub.3                                                                            H       OMe                                                    SCH.sub.2 SCH.sub.3                                                                            H       OCF.sub.2 H                                            SCH.sub.2 SCH.sub.2 CH.sub.3                                                                   H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OMe                                                    S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OMe                                                    SCH(CH.sub.3)SCH.sub.3                                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2                                                           CH.sub.3                                                                               OCF.sub. 2 H                                           SCH.sub.2 SCH.sub.2 CF.sub.3                                                                   H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                         H       OMe                                                    S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                         H       Me                                                     S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                          H       OMe                                                    S(CH.sub.2).sub.2 SCF.sub.3                                                                    H       OCF.sub.2 H                                            SCH.sub.2 CN    H       Me                                                     SCH.sub.2 CN    H       OMe                                                    SCH.sub.2 CN    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CN                                                                           H       Me                                                     S(CH.sub.2).sub.2 CN                                                                           H       OMe                                                    S(CH.sub.2).sub.2 CN                                                                           H       OCF.sub.2 H                                            SCH(CH.sub.3)CN H       Me                                                     SCHF.sub.2      H       OMe                                                    SCHF.sub.2      H       OCF.sub.2 H                                            SCHF.sub.2      CH.sub.3                                                                               Me                                                     SCHF.sub.2      H       Me                                                     SCF.sub.3       H       OMe                                                    SCH.sub.2 CFH.sub.2                                                                            H       OCF.sub.2 H                                            SCH.sub.2 CF.sub.2 H                                                                           H       Me                                                     SCH.sub.2 CF.sub.3                                                                             H       OMe                                                    SCH.sub.2 CF.sub.3                                                                             H       OCF.sub.2 H                                            SCH.sub.2 CF.sub.3                                                                             H       Me                                                     SCH.sub.2 CF.sub.2 H                                                                           H       OMe                                                    S(CH.sub.2).sub.2 CFH.sub.2                                                                    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CClH.sub.2                                                                   CH.sub.3                                                                               OMe                                                    S(CH.sub.2).sub.2 CIH.sub. 2                                                                   H       Me                                                     SCF.sub.2 CF.sub.3                                                                             H       OMe                                                    SCH(CH.sub.3)CF.sub.3                                                                          H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CCl.sub.3                                                                    H       Me                                                     S(O)CHF.sub.2   H       OMe                                                    S(O)CHF.sub.2   H       OCF.sub.2 H                                            S(O)CHF.sub.2   H       Me                                                     S(O)CF.sub.3    H       OMe                                                    S(O)CH.sub.2 CFH.sub.2                                                                         H       OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.2 H                                                                        CH.sub.3                                                                               OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.3                                                                          H       Me                                                     S(O)CH.sub.2 CF.sub.3                                                                          H       OMe                                                    S(O)CH.sub.2 CF.sub.3                                                                          H       OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.2 H                                                                        H       Me                                                     S(O)(CH.sub.2).sub.2 CFH.sub.2                                                                 H       OMe                                                    S(O)(CH.sub.2).sub.2 CClH.sub.2                                                                H       OCF.sub.2 H                                            S(O)(CH.sub.2).sub.2 CIH.sub.2                                                                 H       Me                                                     S(O)CF.sub.2 CF.sub.3                                                                          H       OMe                                                    S(O)CH(CH.sub.3)CF.sub.3                                                                       H       OCF.sub.2 H                                            S(O)(CH.sub.2).sub.2 CCl.sub.3                                                                 H       Me                                                     S(O).sub.2 CHF.sub.2                                                                           H       OMe                                                    S(O).sub.2 CHF.sub.2                                                                           H       OCF.sub.2 H                                            S(O).sub.2 CHR.sub.2                                                                           H       Me                                                     S(O).sub.2 CF.sub.3                                                                            H       OMe                                                    S(O).sub.2 CH.sub.2 CFH.sub.2                                                                  H       OCF.sub.2 H                                            S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                 CH.sub.3                                                                               Me                                                     S(O).sub.2 CH.sub.2 CF.sub.3                                                                   H       Me                                                     S(O).sub.2 CH.sub.2 CF.sub.3                                                                   H       OMe                                                    S(O).sub.2 CH.sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                            S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                 H       Me                                                     S(O).sub.2 (CH.sub.2).sub.2 CFH.sub.2                                                          H       OMe                                                    S(O).sub.2 (CH.sub.2).sub.2 CClH.sub.2                                                         H       OCF.sub.2 H                                            S(O).sub.2 (CH.sub.2).sub.2 CIH.sub.2                                                          H       Me                                                     S(O).sub.2 CF.sub.2 CF.sub.3                                                                   H       OMe                                                    S(O).sub.2 CH(CH.sub.3)CF.sub.3                                                                H       OCF.sub.2 H                                            S(O).sub.2 (CH.sub.2).sub.2 CCl.sub.3                                                          CH.sub.3                                                                               OMe                                                    S(O).sub.2 CH.sub.2 Cl                                                                         H       Me                                                     CH═CH.sub.2 H       OMe                                                    CH═CH.sub.2 H       OCF.sub.2 H                                            CH═CH.sub.2 H       Me                                                     CH.sub.2 CH═CH.sub.2                                                                       H       OMe                                                    CH.sub.2 CH═CH.sub.2                                                                       H       OCF.sub.2 H                                            CH.sub.2 CH═CH.sub.2                                                                       H       Me                                                     CH═CHCH.sub.3                                                                              H       OMe                                                    C(CH.sub.3)═CH.sub.2                                                                       H       OCF.sub.2 H                                            CH═CH.sub.2 CH.sub.3                                                                               OCF.sub.2 H                                            C.tbd.CH        H       Me                                                     C.tbd.CH        H       OMe                                                    C.tbd.CH        H       OCF.sub.2 H                                            CH.sub.2 C.tbd.CH                                                                              H       Me                                                     CH.sub.2 C.tbd.CH                                                                              H       OMe                                                    CH.sub.2 C.tbd.CH                                                                              H       OCF.sub.2 H                                            C.tbd.CCH.sub.3 H       Me                                                     C.tbd.CCH.sub.3 H       OMe                                                    C.tbd.CCH.sub.3 H       OCF.sub.2 H                                            NH.sub.2        H       Me                                                     NH.sub.2        H       OMe                                                    NH.sub.2        H       OCF.sub.2 H                                            NHCH.sub.3      H       Me                                                     NHCH.sub.3      H       OMe                                                    NHCH.sub.3      H       OCF.sub.2 H                                            NHCH.sub.3      CH.sub.3                                                                               Me                                                     N(CH.sub.3).sub.2                                                                              H       Me                                                     N(CH.sub.3).sub.2                                                                              H       OMe                                                    N(CH.sub.3).sub.2                                                                              H       OCF.sub.2 H                                            NHCH.sub.2 CH.sub.3                                                                            H       Me                                                     NHCH.sub.2 CH.sub.3                                                                            H       OMe                                                    NHCH.sub.2 CH.sub.3                                                                            H       OCF.sub.2 H                                            N(CH.sub.3)CH.sub.2 CH.sub.3                                                                   H       Me                                                     N(CH.sub.2 CH.sub.3).sub.2                                                                     H       OMe                                                    NHCH.sub.2 CF.sub.3                                                                            H       OCF.sub.2 H                                            NHCH.sub.2 CF.sub.3                                                                            CH.sub.3                                                                               OMe                                                    NHCH.sub.2 CF.sub.3                                                                            H       Me                                                     NHCH.sub.2 CF.sub.3                                                                            H       OMe                                                    N(CH.sub.3)CH.sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                            N(CH.sub.3)CH.sub.2 CHF.sub.2                                                                  H       Me                                                     N(CH.sub.3)(CH.sub.2).sub.2 F                                                                  H       OMe                                                    N(CH.sub.3)(CH.sub.2).sub.2 Cl                                                                 H       OCF.sub.2 H                                            N(CH.sub.3)(CH.sub.2).sub.2 I                                                                  H       Me                                                     N(CH.sub.3)(CH.sub.2).sub.2 Br                                                                 H       OMe                                                    NHCF.sub.3      CH.sub.3                                                                               OCF.sub.2 H                                            NHCF.sub.3      H       Me                                                     NH(CH.sub.2).sub.2 F                                                                           H       OMe                                                    N(CH.sub.3)CF.sub.2 H                                                                          H       OCF.sub.2 H                                            NHCF.sub.2 H    H       Me                                                     ______________________________________                                    

                  TABLE IlI                                                        ______________________________________                                         R.sub.1 = n-Pr                                                                 R.sub.2       R        Y        m.p. (°C.)                              ______________________________________                                         Me            H        Me                                                      Me            Me       Me                                                      Me            H        OMe                                                     Me            Me       OMe                                                     Me            H        OCF.sub.2 H                                             Me            Me       OCF.sub.2 H                                             Et            H        Me                                                      Et            Me       Me                                                      Et            H        OMe                                                     Et            Me       OMe                                                     Et            H        OCF.sub.2 H                                             Et            Me       OCF.sub.2 H                                              -n-Pr        H        Me                                                       -n-Pr        Me       Me                                                       -n-Pr        H        OMe                                                      -n-Pr        Me       OMe                                                      -n-Pr        H        OCF.sub.2 H                                              -n-Pr        Me       OCF.sub.2 H                                              .sub.-i-Pr   H        Me                                                       .sub.-i-Pr   Me       Me                                                       .sub.-i-Pr   H        OMe                                                      .sub.-i-Pr   Me       OMe                                                      .sub.-i-Pr   H        OCF.sub.2 H                                              .sub.-i-Pr   Me       OCF.sub.2 H                                             cyclo-Pr      H        Me                                                      cyclo-Pr      Me       Me                                                      cyclo-Pr      H        OMe                                                     cyclo-Pr      Me       OMe                                                     cyclo-Pr      H        OCF.sub.2 H                                             cyclo-Pr      Me       OCF.sub.2 H                                             OMe           H        Me                                                      OMe           Me       Me                                                      OMe           H        OMe                                                     OMe           Me       OMe                                                     OMe           H        OCF.sub.2 H                                             OMe           Me       OCF.sub.2 H                                             OEt           H        Me                                                      OEt           Me       Me                                                      OEt           H        OMe                                                     OEt           Me       OMe                                                     OEt           H        OCF.sub.2 H                                             OEt           Me       OCF.sub.2 H                                             O-- -n-Pr     H        Me                                                      O-- -n-Pr     Me       Me                                                      O-- -n-Pr     H        OMe                                                     O-- -n-Pr     Me       OMe                                                     O-- -n-Pr     H        OCF.sub.2 H                                             O-- -n-Pr     Me       OCF.sub.2 H                                             O-- .sub.-i-Pr                                                                               H        Me                                                      O-- .sub.-i-Pr                                                                               Me       Me                                                      O-- .sub.-i-Pr                                                                               H        OMe                                                     O-- .sub.-i-Pr                                                                               Me       OMe                                                     O-- .sub.-i-Pr                                                                               H        OCF.sub.2 H                                             O-- .sub.-i-Pr                                                                               Me       OCF.sub.2 H                                             SMe           H        Me                                                      SMe           Me       Me                                                      SMe           H        OMe      117-121                                        SMe           Me       OMe                                                     SMe           H        OCF.sub.2 H                                             SMe           Me       OCF.sub.2 H                                             SEt           H        Me                                                      SEt           Me       Me                                                      SEt           H        OMe                                                     SEt           Me       OMe                                                     SEt           H        OCF.sub.2 H                                             SEt           Me       OCF.sub.2 H                                             S-- -n-Pr      -n-Pr   H        Me                                             S-- -n-Pr      -n-Pr   Me       Me                                             S-- -n-Pr      -n-Pr   H        OMe                                            S-- -n-Pr      -n-Pr   Me       OMe                                            S-- -n-Pr      -n-Pr   H        OCF.sub.2 H                                    S-- -n-Pr      -n-Pr   Me       OCF.sub.2 H                                    S-- .sub.-i-Pr                                                                                .sub.-i-Pr                                                                             H        Me                                             S-- .sub.-i-Pr                                                                                .sub.-i-Pr                                                                             Me       Me                                             S-- .sub.-i-Pr                                                                                .sub.-i-Pr                                                                             H        OMe                                            S-- .sub.-i-Pr                                                                                .sub.-i-Pr                                                                             Me       OMe                                            S-- .sub.-i-Pr                                                                                .sub.-i-Pr                                                                             H        OCF.sub.2 H                                    S-- .sub.-i-Pr                                                                                .sub.-i-Pr                                                                             Me       OCF.sub.2 H                                    O--allyl      H        Me                                                      O--allyl      Me       Me                                                      O--allyl      H        OMe                                                     O--allyl      Me       OMe                                                     O--allyl      H        OCF.sub.2 H                                             O--allyl      Me       OCF.sub.2 H                                             O--propargyl  H        Me                                                      O--propargyl  Me       Me                                                      O--propargyl  H        OMe                                                     O--propargyl  Me       OMe                                                     O--propargyl  H        OCF.sub.2 H                                             O--propargyl  Me       OCF.sub.2 H                                             CH.sub.2 F    H        Me                                                      CH.sub.2 F    Me       Me                                                      CH.sub.2 F    H        OMe                                                     CH.sub.2 F    Me       OMe                                                     CH.sub.2 F    H        OCF.sub.2 H                                             CH.sub.2 F    Me       OCF.sub.2 H                                             CHF.sub.2     H        Me                                                      CHF.sub.2     Me       Me                                                      CHF.sub.2     H        OMe                                                     CHF.sub.2     Me       OMe                                                     CHF.sub.2     H        OCF.sub.2 H                                             CHF.sub.2     Me       OCF.sub.2 H                                             CF.sub.3      H        Me                                                      CF.sub.3      Me       Me                                                      CF.sub.3      H        OMe                                                     CF.sub.3      Me       OMe                                                     CF.sub.3      H        OCF.sub.2 H                                             CF.sub.3      Me       OCF.sub.2 H                                             CH.sub.2 Cl   H        Me                                                      CH.sub.2 Cl   Me       Me                                                      CH.sub.2 Cl   H        OMe                                                     CH.sub.2 Cl   Me       OMe                                                     CH.sub.2 Cl   H        OCF.sub.2 H                                             CH.sub.2 Cl   Me       OCF.sub.2 H                                             CHCl.sub.2    H        Me                                                      CHCl.sub.2    Me       Me                                                      CHCl.sub.2    H        OMe                                                     CHCl.sub.2    Me       OMe                                                     CHCl.sub.2    H        OCF.sub.2 H                                             CHCl.sub.2    Me       OCF.sub.2 H                                             CCl.sub.3     H        Me                                                      CCl.sub.3     Me       Me                                                      CCl.sub.3     H        OMe                                                     CCl.sub.3     Me       OMe                                                     CCl.sub.3     H        OCF.sub.2 H                                             CCl.sub.3     Me       OCF.sub.2 H                                             CHFCH.sub.3   H        Me                                                      CHFCH.sub.3   Me       Me                                                      CHFCH.sub.3   H        OMe                                                     CHFCH.sub.3   Me       OMe                                                     CHFCH.sub.3   H        OCF.sub.2 H                                             CHFCH.sub.3   Me       OCF.sub.2 H                                             CF.sub.2 CH.sub.3                                                                            H        Me                                                      CF.sub.2 CH.sub.3                                                                            Me       Me                                                      CF.sub.2 CH.sub.3                                                                            H        OMe                                                     CF.sub.2 CH.sub.3                                                                            Me       OMe                                                     CF.sub.2 CH.sub.3                                                                            H        OCF.sub.2 H                                             CF.sub.2 CH.sub.3                                                                            Me       OCF.sub.2 H                                             CH.sub.2 CH.sub.2 F                                                                          H        Me                                                      CH.sub.2 CH.sub.2 F                                                                          Me       Me                                                      CH.sub.2 CH.sub.2 F                                                                          H        OMe                                                     CH.sub.2 CH.sub.2 F                                                                          Me       OMe                                                     CH.sub.2 CH.sub.2 F                                                                          H        OCF.sub.2 H                                             CH.sub.2 CH.sub.2 F                                                                          Me       OCF.sub.2 H                                             CH.sub.2 CHF.sub.2                                                                           H        Me                                                      CH.sub.2 CHF.sub.2                                                                           Me       Me                                                      CH.sub.2 CHF.sub.2                                                                           H        OMe                                                     CH.sub.2 CHF.sub.2                                                                           Me       OMe                                                     CH.sub.2 CHF.sub.2                                                                           H        OCF.sub.2 H                                             CH.sub.2 CHF.sub.2                                                                           Me       OCF.sub.2 H                                             CH.sub.2 CF.sub.3                                                                            H        Me                                                      CH.sub.2 CF.sub.3                                                                            Me       Me                                                      CH.sub.2 CF.sub.3                                                                            H        OMe                                                     CH.sub.2 CF.sub.3                                                                            Me       OMe                                                     CH.sub.2 CF.sub.3                                                                            H        OCF.sub.2 H                                             CH.sub.2 CF.sub.3                                                                            Me       OCF.sub.2 H                                             CHClCH.sub.3  H        Me                                                      CHClCH.sub.3  Me       Me                                                      CHClCH.sub.3  H        OMe                                                     CHClCH.sub.3  Me       OMe                                                     CHClCH.sub.3  H        OCF.sub.2 H                                             CHClCH.sub.3  Me       OCF.sub.2 H                                             CH.sub.2 OCH.sub. 3                                                                          H        Me                                                      CH.sub.2 OCH.sub.3                                                                           Me       Me                                                      CH.sub.2 OCH.sub.3                                                                           H        OHe                                                     CH.sub.2 OCH.sub.3                                                                           Me       OMe                                                     CH.sub.2 OCH.sub.3                                                                           H        OCF.sub.2 H                                             CH.sub.2 OCH.sub.3                                                                           Me       OCF.sub.2 H                                             (CH.sub.2).sub.2 OCH.sub.3                                                                   H        Me                                                      (CH.sub.2).sub.2 OCH.sub.3                                                                   Me       Me                                                      (CH.sub.2).sub.2 OCH.sub.3                                                                   H        OMe                                                     (CH.sub.2).sub.2 OCH.sub.3                                                                   Me       OMe                                                     (CH.sub.2).sub.2 OCH.sub.3                                                                   H        OCF.sub.2 H                                             (CH.sub.2).sub.2 OCH.sub.3                                                                   Me       OCF.sub.2 H                                             CH(OCH.sub.3)CH.sub.3                                                                        H        Me                                                      CH(OCH.sub.3)CH.sub.3                                                                        Me       Me                                                      CH(OCH.sub.3)CH.sub.3                                                                        H        OMe                                                     CH(OCH.sub.3)CH.sub.3                                                                        Me       OMe                                                     CH(OCH.sub.3)CH.sub.3                                                                        H        OCF.sub.2 H                                             CH(OCH.sub.3)CH.sub.3                                                                        Me       OCF.sub.2 H                                             CH.sub.2 SCH.sub.3                                                                           H        Me                                                      CH.sub.2 SCH.sub.3                                                                           Me       Me                                                      CH.sub.2 SCH.sub.3                                                                           H        OMe                                                     CH.sub.2 SCH.sub.3                                                                           Me       OMe                                                     CH.sub.2 SCH.sub.3                                                                           H        OCF.sub.2 H                                             CH.sub.2 SCH.sub.3                                                                           Me       OCF.sub.2 H                                             (CH.sub.2).sub.2 SCH.sub.3                                                                   H        Me                                                      (CH.sub.2).sub.2 SCH.sub.3                                                                   Me       Me                                                      (CH.sub.2).sub.2 SCH.sub.3                                                                   H        OMe                                                     (CH.sub.2).sub.2 SCH.sub.3                                                                   Me       OMe                                                     (CH.sub.2).sub.2 SCH.sub.3                                                                   H        OCF.sub.2 H                                             (CH.sub.2).sub.2 SCH.sub.3                                                                   Me       OCF.sub.2 H                                             CH(SCH.sub.3)CH.sub.3                                                                        H        Me                                                      CH(SCH.sub.3)CH.sub.3                                                                        Me       Me                                                      CH(SCH.sub.3)CH.sub.3                                                                        H        OMe                                                     CH(SCH.sub.3)CH.sub.3                                                                        Me       OMe                                                     CH(SCH.sub.3)CH.sub.3                                                                        H        OCF.sub.2 H                                             CH(SCH.sub.3)CH.sub.3                                                                        Me       OCF.sub.2 H                                             OCF.sub.2 H   H        Me                                                      OCF.sub.2 H   Me       Me                                                      OCF.sub.2 H   H        OMe                                                     OCF.sub.2 H   Me       OMe                                                     OCF.sub.2 H   H        OCF.sub.2 H                                             OCF.sub.2 H   Me       OCF.sub.2 H                                             OCH.sub.2 CH.sub.2 F                                                                         H        Me                                                      OCH.sub.2 CH.sub.2 F                                                                         Me       Me                                                      OCH.sub.2 CH.sub.2 F                                                                         H        OMe                                                     OCH.sub.2 CH.sub.2 F                                                                         Me       OMe                                                     OCH.sub.2 CH.sub.2 F                                                                         H        OCF.sub.2 H                                             OCH.sub.2 CH.sub.2 F                                                                         Me       OCF.sub.2 H                                             OCH.sub.2 CHF.sub.2                                                                          H        Me                                                      OCH.sub.2 CHF.sub.2                                                                          Me       Me                                                      OCH.sub.2 CHF.sub.2                                                                          H        OMe                                                     OCH.sub.2 CHF.sub.2                                                                          Me       OMe                                                     OCH.sub.2 CHF.sub.2                                                                          H        OCF.sub.2 H                                             OCH.sub.2 CHF.sub.2                                                                          Me       OCF.sub.2 H                                             OCH.sub.2 CF.sub.3                                                                           H        Me                                                      OCH.sub.2 CF.sub.3                                                                           Me       Me                                                      OCH.sub.2 CF.sub.3                                                                           H        OMe                                                     OCH.sub.2 CF.sub.3                                                                           Me       OMe                                                     OCH.sub.2 CF.sub.3                                                                           H        OCF.sub.2 H                                             OCH.sub.2 CF.sub.3                                                                           Me       OCF.sub.2 H                                             O(CH.sub.2).sub.2 Cl                                                                         H        Me                                                      O(CH.sub.2).sub.2 Cl                                                                         Me       Me                                                      O(CH.sub.2).sub.2 Cl                                                                         H        OMe                                                     O(CH.sub.2).sub.2 Cl                                                                         Me       OMe                                                     O(CH.sub.2).sub.2 Cl                                                                         H        OCF.sub.2 H                                             O(CH.sub.2).sub.2 Cl                                                                         Me       OCF.sub.2 H                                             S(O)Me        H        Me                                                      S(O)Me        Me       Me                                                      S(O)Me        H        OMe                                                     S(O)Me        Me       OMe                                                     S(O)Me        H        OCF.sub.2 H                                             S(O)Me        Me       OCF.sub.2 H                                             S(O)Et        H        Me                                                      S(O)Et        Me       Me                                                      S(O)Et        H        OMe                                                     S(O)Et        Me       OMe                                                     S(O)Et        H        OCF.sub.2 H                                             S(O)Et        Me       OCF.sub.2 H                                             S(O)-- -n-Pr  H        Me                                                      S(O)-- -n-Pr  Me       Me                                                      S(O)-- -n-Pr  H        OMe                                                     S(O)-- -n-Pr  Me       OMe                                                     S(O)-- -n-Pr  H        OCF.sub.2 H                                             S(O)-- -n-Pr  Me       OCF.sub.2 H                                             S(O)-- .sub.-i-Pr                                                                            H        Me                                                      S(O)-- .sub.-i-Pr                                                                            Me       Me                                                      S(O)-- .sub.-i-Pr                                                                            H        OMe                                                     S(O)-- .sub.-i-Pr                                                                            Me       Me                                                      S(O)-- .sub.-i-Pr                                                                            H        OCF.sub.2 H                                             S(O)-- .sub.-i-Pr                                                                            Me       OCF.sub.2 H                                             SO.sub.2 Me   H        Me                                                      SO.sub.2 Me   Me       Me                                                      SO.sub.2 Me   H        OMe                                                     SO.sub.2 Me   Me       OMe                                                     SO.sub.2 Me   H        OCF.sub.2 H                                             SO.sub.2 Me   Me       OCF.sub.2 H                                             SO.sub.2 Et   H        Me                                                      SO.sub.2 Et   Me       Me                                                      SO.sub.2 Et   H        OMe                                                     SO.sub.2 Et   Me       OMe                                                     SO.sub.2 Et   H        OCF.sub.2 H                                             SO.sub.2 Et   Me       OCF.sub.2 H                                             SO.sub.2 -- -n-Pr                                                                            H        Me                                                      SO.sub.2 -- -n-Pr                                                                            Me       Me                                                      SO.sub.2 -- -n-Pr                                                                            H        OMe                                                     SO.sub.2 -- -n-Pr                                                                            Me       OMe                                                     SO.sub.2 -- -n-Pr                                                                            H        OCF.sub.2 H                                             SO.sub.2 -- -n-Pr                                                                            Me       OCF.sub.2 H                                             SO.sub.2 -- .sub.-i-Pr                                                                       H        Me                                                      SO.sub.2 -- .sub.-i-Pr                                                                       Me       Me                                                      SO.sub.2 -- .sub.-i-Pr                                                                       H        OMe                                                     SO.sub.2 -- .sub.-i-Pr                                                                       Me       OMe                                                     SO.sub.2 -- .sub.-i-Pr                                                                       H        OCF.sub.2 H                                             SO.sub.2 -- .sub.-i-Pr                                                                       Me       OCF.sub. 2 H                                            S--allyl      H        Me                                                      S--allyl      Me       Me                                                      S--allyl      H        OMe                                                     S--allyl      Me       OMe                                                     S--allyl      H        OCF.sub.2 H                                             S--allyl      Me       OCF.sub.2 H                                             S(O)allyl     H        Me                                                      S(O)allyl     Me       Me                                                      S(O)allyl     H        OMe                                                     S(O)allyl     Me       OMe                                                     S(O)allyl     H        OCF.sub.2 H                                             S(O)allyl     Me       OCF.sub.2 H                                             SO.sub.2 allyl                                                                               H        Me                                                      SO.sub.2 allyl                                                                               Me       Me                                                      SO.sub.2 allyl                                                                               H        OMe                                                     SO.sub.2 allyl                                                                               Me       OMe                                                     SO.sub.2 allyl                                                                               H        OCF.sub.2 H                                             SO.sub.2 allyl                                                                               Me       OCF.sub.2 H                                             S--propargyl  H        Me                                                      S--propargyl  Me       Me                                                      S--propargyl  H        OMe                                                     S--propargyl  Me       OMe                                                     S--propargyl  H        OCF.sub.2 H                                             S--propargyl Me                                                                              OCF.sub.2 H                                                      S(O)propargyl H        Me                                                      S(O)propargyl Me       Me                                                      S(O)propargyl H        OMe                                                     S(O)propargyl Me       OMe                                                     S(O)propargyl H        OCF.sub.2 H                                             S(O)propargyl Me       OCF.sub.2 H                                             SO.sub.2 propargyl                                                                           H        Me                                                      SO.sub.2 propargyl                                                                           Me       Me                                                      SO.sub.2 propargyl                                                                           H        OMe                                                     SO.sub.2 propargyl                                                                           Me       OMe                                                     SO.sub.2 propargyl                                                                           H        OCF.sub.2 H                                             SO.sub.2 propargyl                                                                           Me       OCF.sub.2 H                                             ______________________________________                                    

                  TABLE IIIa                                                       ______________________________________                                         R.sub.1 = n-Pr                                                                 R.sub.2          R       Y         m.p. (°C.)                           ______________________________________                                         CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       Me                                                    CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       OMe                                                   CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       Me                                                    (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       OMe                                                   (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             CH.sub.3                                                                               Me                                                    CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                  H       Me                                                    CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       Me                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                     H       OMe                                                   CH.sub.2 OCH.sub.2 CF.sub.3                                                                     H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                           H       Me                                                    (CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                             H       OMe                                                   CH.sub.2 OCF.sub.2 H                                                                            H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                   CH.sub.3                                                                               OMe                                                   CH.sub.2 OCH.sub.2 CHF.sub.2                                                                    H       Me                                                    CH.sub.2 OCH.sub. 2 CH.sub.2 Br                                                                 H       OMe                                                   CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                  H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.2 I                                                                   H       Me                                                    CH.sub.2 OCF.sub.3                                                                              H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       Me                                                    CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       OMe                                                   (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             H       OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             CH.sub.3                                                                               OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             H       Me                                                    (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             H       OMe                                                   CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       Me                                                    CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       Me                                                    CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       OMe                                                   (CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                           H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                   H       OMe                                                   CH(CH.sub.3)S(O).sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           CH.sub.3                                                                               Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                 H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                   H       OMe                                                   CH.sub.2 S(O).sub.2 CF.sub.2 H                                                                  H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 F                                                         H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CHF.sub.2                                                          H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 Br                                                        H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 I                                                         CH.sub.3                                                                               OMe                                                   CH.sub.2 S(O).sub.2 CF.sub.3                                                                    H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                 H       OMe                                                   OCH.sub.2 OCH.sub.3                                                                             H       OCF.sub.2 H                                           OCH.sub.2 OCH.sub.3                                                                             H       Me                                                    OCH.sub.2 OCH.sub.3                                                                             H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       Me                                                    O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            CH.sub.3                                                                               OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       Me                                                    O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OMe                                                   OCH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                             H       Me                                                    CH.sub.2 SCF.sub.2 H                                                                            H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.2 F                                                                   H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CHF.sub.2                                                                    H       Me                                                    CH.sub.2 SCH.sub.2 CH.sub.2 Br                                                                  H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.2 Cl                                                                  H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CH.sub.2 I                                                                   CH.sub.3                                                                               Me                                                    CH.sub.2 SCF.sub.3                                                                              H       Me                                                    CH.sub.2 S(O)CH.sub.3                                                                           H       OMe                                                   CH.sub.2 S(O)CH.sub.3                                                                           H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.3                                                                           H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       OMe                                                   (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       Me                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  CH.sub.3                                                                               OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                          H       OMe                                                   CH(CH.sub.3)S(O)CH.sub.3                                                                        H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                  H       Me                                                    CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                  H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                  H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                        H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                          H       OMe                                                   CH.sub.2 S(O)CF.sub.2 H                                                                         H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CH.sub.2 F                                                                CH.sub.3                                                                               OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CHF.sub.2                                                                 H       Me                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.2 Br                                                               H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.2 I                                                                H       OCF.sub.2 H                                           CH.sub.2 S(O)CF.sub.3                                                                           H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       OMe                                                   (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           OCH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       Me                                                    O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                          H       Me                                                    O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                          H       OMe                                                   O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                           H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCF.sub.3                                                                     H       Me                                                    OCH.sub.2 SCH.sub.3                                                                             H       OMe                                                   OCH.sub.2 SCH.sub.3                                                                             H       OCF.sub.2 H                                           OCH.sub.2 SCH.sub.3                                                                             H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OMe                                                   O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 SCH.sub.3                                                                     CH.sub.3                                                                               Me                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                   O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       Me                                                    OCH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OMe                                                   OCH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OMe                                                   O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                          H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                          CH.sub.3                                                                               OMe                                                   O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                           H       Me                                                    O(CH.sub.2).sub.2 SCF.sub.3                                                                     H       OMe                                                   OCH.sub.2 S(O)CH.sub.3                                                                          H       OCF.sub.2 H                                           OCH.sub.2 S(O)CH.sub.3                                                                          H       Me                                                    OCH.sub.2 S(O)CH.sub.3                                                                          H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       Me                                                    O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         CH.sub.3                                                                               OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         H       Me                                                    OCH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                         H       OCF.sub.2 H                                           OCH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       Me                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                       H       OMe                                                   O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Cl                                                       H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Br                                                       H       Me                                                    O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 I                                                        H       OMe                                                   O(CH.sub.2).sub.2 S(O)CF.sub. 3                                                                 H       OCF.sub.2 H                                           OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OMe                                                   OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  CH.sub.3                                                                               Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OCF.sub.2 H                                           OCH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                  H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Cl                                                H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Br                                                H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 I                                                 CH.sub.3                                                                               OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CF.sub.3                                                           H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                H       OMe                                                   OCH.sub.2 S(O).sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 CN                                                                            H       Me                                                    O(CH.sub.2).sub.2 CN                                                                            H       OMe                                                   O(CH.sub.2).sub.2 CN                                                                            H       OCF.sub.2 H                                           OCH.sub.2 CN     H       Me                                                    OCH.sub.2 CN     H       OMe                                                   OCH.sub.2 CN     H       OCF.sub.2 H                                           OCH.sub.2 CN     CH.sub.3                                                                               OCF.sub.2 H                                           OCH(CH.sub.3)CN  H       Me                                                    O(CH.sub.2).sub.2 NH.sub.2                                                                      H       OMe                                                   O(CH.sub.2).sub.2 NH.sub.2                                                                      H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 NH.sub.2                                                                      H       Me                                                    O(CH.sub.2).sub.2 NHCH.sub.3                                                                    H       OMe                                                   O(CH.sub.2).sub.2 NHCH.sub.3                                                                    H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 NHCH.sub.3                                                                    H       Me                                                    O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       OMe                                                   O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       Me                                                    SCH.sub.2 OCH.sub.3                                                                             H       OMe                                                   SCH.sub.2 OCH.sub.3                                                                             H       OCF.sub.2 H                                           SCH.sub.2 OCH.sub.3                                                                             H       Me                                                    SCH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OMe                                                   S(CH.sub.2).sub. 2 OCH.sub.3                                                                    H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 OCH.sub.3                                                                     CH.sub.3                                                                               Me                                                    S(CH.sub.2).sub.2 OCH.sub.3                                                                     H       Me                                                    S(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OMe                                                   S(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       Me                                                    SCH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       OMe                                                   S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                          H       Me                                                    S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                          H       OMe                                                   S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                           H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 OCF.sub.3                                                                     CH.sub.3                                                                               OMe                                                   SCH.sub.2 SCH.sub.3                                                                             H       Me                                                    SCH.sub.2 SCH.sub.3                                                                             H       OMe                                                   SCH.sub.2 SCH.sub.3                                                                             H       OCF.sub.2 H                                           SCH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OMe                                                   S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                   SCH(CH.sub.3)SCH.sub.3                                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            CH.sub. 3                                                                              OCF.sub.2 H                                           SCH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OMe                                                   S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                          H       Me                                                    S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                           H       OMe                                                   S(CH.sub.2).sub.2 SCF.sub.3                                                                     H       OCF.sub.2 H                                           SCH.sub.2 CN     H       Me                                                    SCH.sub.2 CN     H       OMe                                                   SCH.sub.2 CN     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CN                                                                            H       Me                                                    S(CH.sub.2).sub.2 CN                                                                            H       OMe                                                   S(CH.sub.2).sub.2 CN                                                                            H       OCF.sub.2 H                                           SCH(CH.sub.3)CN  H       Me                                                    SCHF.sub.2       H       OMe                                                   SCHF.sub.2       H       OCF.sub.2 H                                           SCHF.sub.2       CH.sub.3                                                                               Me                                                    SCHF.sub.2       H       Me                                                    SCF.sub.3        H       OMe                                                   SCH.sub.2 CFH.sub.2                                                                             H       OCF.sub.2 H                                           SCH.sub.2 CF.sub.2 H                                                                            H       Me                                                    SCH.sub.2 CF.sub.3                                                                              H       OMe                                                   SCH.sub.2 CF.sub.3                                                                              H       OCF.sub.2 H                                           SCH.sub.2 CF.sub.3                                                                              H       Me                                                    SCH.sub.2 CF.sub.2 H                                                                            H       OMe                                                   S(CH.sub.2).sub.2 CFH.sub.2                                                                     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CClH.sub.2                                                                    CH.sub.3                                                                               OMe                                                   S(CH.sub.2).sub. 2 CIH.sub.2                                                                    H       Me                                                    SCF.sub.2 CF.sub.3                                                                              H       OMe                                                   SCH(CH.sub.3)CF.sub.3                                                                           H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CCl.sub.3                                                                     H       Me                                                    S(O)CHF.sub.2    H       OMe                                                   S(O)CHF.sub.2    H       OCF.sub.2 H                                           S(O)CHF.sub.2    H       Me                                                    S(O)CF.sub.3     H       OMe                                                   S(O)CH.sub.2 CFH.sub.2                                                                          H       OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.2 H                                                                         CH.sub.3                                                                               OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.3                                                                           H       Me                                                    S(O)CH.sub.2 CF.sub.3                                                                           H       OMe                                                   S(O)CH.sub.2 CF.sub.3                                                                           H       OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.2 H                                                                         H       Me                                                    S(O)(CH.sub.2).sub.2 CFH.sub.2                                                                  H       OMe                                                   S(O)(CH.sub.2).sub.2 CClH.sub.2                                                                 H       OCF.sub.2 H                                           S(O)(CH.sub.2).sub.2 CIH.sub.2                                                                  H       Me                                                    S(O)CF.sub.2 CF.sub.3                                                                           H       OMe                                                   S(O)CH(CH.sub.3)CF.sub.3                                                                        H       OCF.sub.2 H                                           S(O)(CH.sub.2).sub.2 CCl.sub.3                                                                  H       Me                                                    S(O).sub.2 CHF.sub.2                                                                            H       OMe                                                   S(O).sub.2 CHF.sub.2                                                                            H       OCF.sub.2 H                                           S(O).sub.2 CHF.sub.2                                                                            H       Me                                                    S(O).sub.2 CF.sub.3                                                                             H       OMe                                                   S(O).sub.2 CH.sub.2 CFH.sub.2                                                                   H       OCF.sub.2 H                                           S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                  CH.sub.3                                                                               Me                                                    S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       Me                                                    S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       OMe                                                   S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                  H       Me                                                    S(O).sub.2 (CH.sub.2).sub.2 CFH.sub.2                                                           H       OMe                                                   S(O).sub.2 (CH.sub.2).sub.2 CClH.sub.2                                                          H       OCF.sub.2 H                                           S(O).sub.2 (CH.sub.2).sub.2 ClH.sub.2                                                           H       Me                                                    S(O).sub.2 CF.sub.2 CF.sub.3                                                                    H       OMe                                                   S(O).sub.2 CH(CH.sub.3)CF.sub.3                                                                 H       OCF.sub.2 H                                           S(O).sub.2 (CH.sub.2).sub.2 CCl.sub.3                                                           CH.sub.3                                                                               OMe                                                   S(O).sub.2 CH.sub.2 Cl                                                                          H       Me                                                    CH═CH.sub.2  H       OMe                                                   CH═CH.sub.2  H       OCF.sub.2 H                                           CH═CH.sub.2  H       Me                                                    CH.sub.2 CH═CH.sub.2                                                                        H       OMe                                                   CH.sub.2 CH═CH.sub.2                                                                        H       OCF.sub.2 H                                           CH.sub.2 CH═CH.sub.2                                                                        H       Me                                                    CH═CHCH.sub.3                                                                               H       OMe                                                   C(CH.sub.3)═CH.sub.2                                                                        H       OCF.sub.2 H                                           CH═CH.sub.2  CH.sub.3                                                                               OCF.sub.2 H                                           C.tbd.CH         H       Me                                                    C.tbd.CH         H       OMe                                                   C.tbd.CH         H       OCF.sub.2 H                                           CH.sub.2 C.tbd.CH                                                                               H       Me                                                    CH.sub.2 C.tbd.CH                                                                               H       OMe                                                   CH.sub.2 C.tbd.CH                                                                               H       OCF.sub.2 H                                           C.tbd.CCH.sub.3  H       Me                                                    C.tbd.CCH.sub.3  H       OMe                                                   C.tbd.CCH.sub.3  H       OCF.sub.2 H                                           NH.sub.2         H       Me                                                    NH.sub.2         H       OMe                                                   NH.sub.2         H       OCF.sub.2 H                                           NHCH.sub.3       H       Me                                                    NHCH.sub.3       H       OMe                                                   NHCH.sub.3       H       OCF.sub.2 H                                           NHCH.sub.3       CH.sub.3                                                                               Me                                                    N(CH.sub.3).sub.2                                                                               H       Me                                                    N(CH.sub.3).sub.2                                                                               H       OMe                                                   N(CH.sub.3).sub.2                                                                               H       OCF.sub.2 H                                           NHCH.sub.2 CH.sub.3                                                                             H       Me                                                    NHCH.sub.2 CH.sub.3                                                                             H       OMe                                                   NHCH.sub.2 CH.sub.3                                                                             H       OCF.sub.2 H                                           N(CH.sub.3)CH.sub.2 CH.sub.3                                                                    H       Me                                                    N(CH.sub.2 CH.sub.3).sub.2                                                                      H       OMe                                                   NHCH.sub.2 CF.sub.3                                                                             H       OCF.sub.2 H                                           NHCH.sub.2 CF.sub.3                                                                             CH.sub.3                                                                               OMe                                                   NHCH.sub.2 CF.sub.3                                                                             H       Me                                                    NHCH.sub.2 CF.sub.3                                                                             H       OMe                                                   N(CH.sub.3)CH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           N(CH.sub.3)CH.sub.2 CHF.sub.2                                                                   H       Me                                                    N(CH.sub.3)(CH.sub.2).sub.2 F                                                                   H       OMe                                                   N(CH.sub.3)(CH.sub.2).sub.2 Cl                                                                  H       OCF.sub.2 H                                           N(CH.sub.3)(CH.sub.2).sub.2 I                                                                   H       Me                                                    N(CH.sub.3)(CH.sub.2).sub.2 Br                                                                  H       OMe                                                   NHCF.sub.3       CH.sub.3                                                                               OCF.sub.2 H                                           NHCF.sub.3       H       Me                                                    NH(CH.sub.2).sub.2 F                                                                            H       OMe                                                   N(CH.sub.3)CF.sub.2 H                                                                           H       OCF.sub.2 H                                           NHCF.sub. 2 H    H       Me                                                    ______________________________________                                    

                  TABLE IV                                                         ______________________________________                                         R.sub.1 =  .sub.-i-Pr                                                          R.sub.2      R        Y        m.p. (°C.)                               ______________________________________                                         Me           H        Me       173-175                                         Me           Me       Me                                                       Me           H        OMe      173-175                                         Me           Me       OMe                                                      Me           H        OCF.sub.2 H                                              Me           Me       OCF.sub.2 H                                              Et           H        Me                                                       Et           Me       Me                                                       Et           H        OMe                                                      Et           Me       OMe                                                      Et           H        OCF.sub.2 H                                              Et           Me       OCF.sub.2 H                                               -n-Pr       H        Me                                                        -n-Pr       Me       Me                                                        -n-Pr       H        OMe                                                       -n-Pr       Me       OMe                                                       -n-Pr       H        OCF.sub.2 H                                               -n-Pr       Me       OCF.sub.2 H                                               .sub.-i-Pr  H        Me                                                        .sub.-i-Pr  Me       Me                                                        .sub.-i-Pr  H        OMe                                                       .sub.-i-Pr  Me       OMe                                                       .sub.-i-Pr  H        OCF.sub.2 H                                               .sub.-i-Pr  Me       OCF.sub.2 H                                              cyclo-Pr     H        Me                                                       cyclo-Pr     Me       Me                                                       cyclo-Pr     H        OMe                                                      cyclo-Pr     Me       OMe                                                      cyclo-Pr     H        OCF.sub.2 H                                              cyclo-Pr     Me       OCF.sub.2 H                                              OMe          H        Me       128-132                                         OMe          Me       Me                                                       OMe          H        OMe      178-183                                         OMe          Me       OMe                                                      OMe          H        OCF.sub.2 H                                              OMe          Me       OCF.sub.2 H                                              OEt          H        Me                                                       OEt          Me       Me                                                       OEt          H        OMe                                                      OEt          Me       OMe                                                      OEt          H        OCF.sub.2 H                                              OEt          Me       OCF.sub.2 H                                              O-- -n-Pr    H        Me                                                       O-- -n-Pr    Me       Me                                                       O-- -n-Pr    H        OMe                                                      O-- -n-Pr    Me       OMe                                                      O-- -n-Pr    H        OCF.sub.2 H                                              O-- -n-Pr    Me       OCF.sub.2 H                                              O-- .sub.-i-Pr                                                                              H        Me                                                       O-- .sub.-i-Pr                                                                              Me       Me                                                       O-- .sub.-i-Pr                                                                              H        OMe                                                      O-- .sub.-i-Pr                                                                              Me       OMe                                                      O-- .sub.-i-Pr                                                                              H        OCF.sub.2 H                                              O-- .sub.-i-Pr                                                                              Me       OCF.sub.2 H                                              SMe          H        Me       163-165                                         SMe          Me       Me                                                       SMe          H        OMe      127-131                                         SMe          Me       OMe                                                      SMe          H        OCF.sub.2 H                                              SMe          Me       OCF.sub.2 H                                              SEt          H        Me                                                       SEt          Me       Me                                                       SEt          H        OMe                                                      SEt          Me       OMe                                                      SEt          H        OCF.sub.2 H                                              SEt          Me       OCF.sub.2 H                                              S-- -n-Pr    H        Me                                                       S-- -n-Pr    Me       Me                                                       S-- -n-Pr    H        OMe                                                      S-- -n-Pr    Me       OMe                                                      S-- -n-Pr    H        OCF.sub.2 H                                              S-- -n-Pr    Me       OCF.sub.2 H                                              S-- .sub.-i-Pr                                                                              H        Me                                                       S-- .sub.-i-Pr                                                                              Me       Me                                                       S-- .sub.-i-Pr                                                                              H        OMe                                                      S-- .sub.-i-Pr                                                                              Me       OMe                                                      S-- .sub.-i-Pr                                                                              H        OCF.sub.2 H                                              S-- .sub.-i-Pr                                                                              Me       OCF.sub.2 H                                              O--allyl     H        Me                                                       O-- allyl    Me       Me                                                       O--allyl     H        OMe                                                      O--allyl     Me       OMe                                                      O--allyl     H        OCF.sub.2 H                                              O--allyl     Me       OCF.sub.2 H                                              O--propargyl H        Me                                                       O--propargyl Me       Me                                                       O--propargyl H        OMe                                                      O--propargyl Me       OMe                                                      O--propargyl H        OCF.sub.2 H                                              O--propargyl Me       OCF.sub.2 H                                              CH.sub.2 F   H        Me                                                       CH.sub.2 F   Me       Me                                                       CH.sub.2 F   H        OMe                                                      CH.sub.2 F   Me       OMe                                                      CH.sub.2 F   H        OCF.sub.2 H                                              CH.sub.2 F   Me       OCF.sub.2 H                                              CHF.sub.2    H        Me                                                       CHF.sub.2    Me       Me                                                       CHF.sub.2    H        OMe                                                      CHF.sub.2    Me       OMe                                                      CHF.sub.2    H        OCF.sub.2 H                                              CHF.sub.2    Me       OCF.sub.2 H                                              CF.sub.3     H        Me       143-146                                         CF.sub.3     Me       Me                                                       CF.sub.3     H        OMe      137-141                                         CF.sub.3     Me       OMe                                                      CF.sub.3     H        OCF.sub.2 H                                              CF.sub.3     Me       OCF.sub.2 H                                              CH.sub.2 Cl  H        Me                                                       CH.sub.2 Cl  Me       Me                                                       CH.sub.2 Cl  H        OMe                                                      CH.sub.2 Cl  Me       OMe                                                      CH.sub.2 Cl  H        OCF.sub.2 H                                              CH.sub.2 Cl  Me       OCF.sub.2 H                                              CHCl.sub.2   H        Me                                                       CHCl.sub.2   Me       Me                                                       CHCl.sub.2   H        OMe                                                      CHCl.sub.2   Me       OMe                                                      CHCl.sub.2   H        OCF.sub.2 H                                              CHCl.sub.2   Me       OCF.sub.2 H                                              CCl.sub.3    H        Me                                                       CCl.sub.3    Me       Me                                                       CCl.sub.3    H        OMe                                                      CCl.sub.3    Me       OMe                                                      CCl.sub.3    H        OCF.sub.2 H                                              CCl.sub.3    Me       OCF.sub.2 H                                              CHFCH.sub.3  H        Me                                                       CHFCH.sub.3  Me       Me                                                       CHFCH.sub.3  H        OMe                                                      CHFCH.sub.3  Me       OMe                                                      CHFCH.sub.3  H        OCF.sub.2 H                                              CHFCH.sub.3  Me       OCF.sub.2 H                                              CF.sub.2 CH.sub.3                                                                           H        Me                                                       CF.sub.2 CH.sub.3                                                                           Me       Me                                                       CF.sub.2 CH.sub.3                                                                           H        OMe                                                      CF.sub.2 CH.sub.3                                                                           Me       OMe                                                      CF.sub.2 CH.sub.3                                                                           H        OCF.sub.2 H                                              CF.sub.2 CH.sub.3                                                                           Me       OCF.sub.2 H                                              CH.sub.2 CH.sub.2 F                                                                         H        Me                                                       CH.sub.2 CH.sub.2 F                                                                         Me       Me                                                       CH.sub.2 CH.sub.2 F                                                                         H        OMe                                                      CH.sub.2 CH.sub.2 F                                                                         Me       OMe                                                      CH.sub.2 CH.sub.2 F                                                                         H        OCF.sub.2 H                                              CH.sub.2 CH.sub.2 F                                                                         Me       OCF.sub.2 H                                              CH.sub.2 CHF.sub.2                                                                          H        Me                                                       CH.sub.2 CHF.sub.2                                                                          Me       Me                                                       CH.sub.2 CHF.sub.2                                                                          H        OMe                                                      CH.sub.2 CHF.sub.2                                                                          Me       OMe                                                      CH.sub.2 CHF.sub.2                                                                          H        OCF.sub.2 H                                              CH.sub.2 CHF.sub.2                                                                          Me       OCF.sub.2 H                                              CH.sub.2 CF.sub.3                                                                           H        Me                                                       CH.sub.2 CF.sub.3                                                                           Me       Me                                                       CH.sub.2 CF.sub.3                                                                           H        OMe                                                      CH.sub.2 CF.sub.3                                                                           Me       OMe                                                      CH.sub.2 CF.sub.3                                                                           H        OCF.sub.2 H                                              CH.sub.2 CF.sub.3                                                                           Me       OCF.sub.2 H                                              CHClCH.sub.3 H        Me                                                       CHClCH.sub.3 Me       Me                                                       CHClCH.sub.3 H        OMe                                                      CHClCH.sub.3 Me       OMe                                                      CHClCH.sub.3 H        OCF.sub.2 H                                              CHClCH.sub.3 Me       OCF.sub.2 H                                              CH.sub.2 OCH.sub.3                                                                          H        Me                                                       CH.sub.2 OCH.sub.3                                                                          Me       Me                                                       CH.sub.2 OCH.sub.3                                                                          H        OMe                                                      CH.sub.2 OCH.sub.3                                                                          Me       OMe                                                      CH.sub.2 OCH.sub.3                                                                          H        OCF.sub.2 H                                              CH.sub.2 OCH.sub.3                                                                          Me       OCF.sub.2 H                                              (CH.sub.2).sub.2 OCH.sub.3                                                                  H        Me                                                       (CH.sub.2).sub.2 OCH.sub.3                                                                  Me       Me                                                       (CH.sub.2).sub.2 OCH.sub.3                                                                  H        OMe                                                      (CH.sub.2).sub.2 OCH.sub.3                                                                  Me       OMe                                                      (CH.sub.2).sub.2 OCH.sub.3                                                                  H        OCF.sub.2 H                                              (CH.sub.2).sub.2 OCH.sub.3                                                                  Me       OCF.sub.2 H                                              CH(OCH.sub.3 )CH.sub.3                                                                      H        Me                                                       CH(OCH.sub.3)CH.sub.3                                                                       Me       Me                                                       CH(OCH.sub.3)CH.sub.3                                                                       H        OMe                                                      CH(OCH.sub.3)CH.sub.3                                                                       Me       OMe                                                      CH(OCH.sub.3)CH.sub.3                                                                       H        OCF.sub.2 H                                              CH(OCH.sub.3)CH.sub.3                                                                       Me       OCF.sub.2 H                                              CH.sub.2 SCH.sub.3                                                                          H        Me                                                       CH.sub.2 SCH.sub.3                                                                          Me       Me                                                       CH.sub.2 SCH.sub.3                                                                          H        OMe                                                      CH.sub.2 SCH.sub.3                                                                          Me       OMe                                                      CH.sub.2 SCH.sub.3                                                                          H        OCF.sub.2 H                                              CH.sub.2 SCH.sub.3                                                                          Me       OCF.sub.2 H                                              (CH.sub.2).sub.2 SCH.sub.3                                                                  H        Me                                                       (CH.sub.2).sub.2 SCH.sub.3                                                                  Me       Me                                                       (CH.sub.2).sub.2 SCH.sub.3                                                                  H        OMe                                                      (CH.sub.2).sub.2 SCH.sub.3                                                                  Me       OMe                                                      (CH.sub.2).sub.2 SCH.sub.3                                                                  H        OCF.sub.2 H                                              (CH.sub.2).sub.2 SCH.sub.3                                                                  Me       OCF.sub.2 H                                              CH(SCH.sub.3)CH.sub.3                                                                       H        Me                                                       CH(SCH.sub.3)CH.sub.3                                                                       Me       Me                                                       CH(SCH.sub.3)CH.sub.3                                                                       H        OMe                                                      CH(SCH.sub.3)CH.sub.3                                                                       Me       OMe                                                      CH(SCH.sub.3)CH.sub.3                                                                       H        OCF.sub.2 H                                              CH(SCH.sub.3)CH.sub.3                                                                       Me       OCF.sub.2 H                                              OCF.sub.2 H  H        Me                                                       OCF.sub.2 H  Me       Me                                                       OCF.sub.2 H  H        OMe                                                      OCF.sub.2 H  Me       OMe                                                      OCF.sub.2 H  H        OCF.sub.2 H                                              OCF.sub.2 H  Me       OCF.sub.2 H                                              OCH.sub.2 CH.sub.2 F                                                                        H        Me                                                       OCH.sub.2 CH.sub.2 F                                                                        Me       Me                                                       OCH.sub.2 CH.sub.2 F                                                                        H        OMe                                                      OCH.sub.2 CH.sub.2 F                                                                        Me       OMe                                                      OCH.sub.2 CH.sub.2 F                                                                        H        OCF.sub.2 H                                              OCH.sub.2 CH.sub.2 F                                                                        Me       OCF.sub.2 H                                              OCH.sub.2 CHF.sub.2                                                                         H        Me                                                       OCH.sub.2 CHF.sub.2                                                                         Me       Me                                                       OCH.sub.2 CHF.sub.2                                                                         H        OMe                                                      OCH.sub.2 CHF.sub.2                                                                         Me       OMe                                                      OCH.sub.2 CHF.sub.2                                                                         H        OCF.sub.2 H                                              OCH.sub.2 CHF.sub.2                                                                         Me       OCF.sub.2 H                                              OCH.sub.2 CF.sub.3                                                                          H        Me                                                       OCH.sub.2 CF.sub.3                                                                          Me       Me                                                       OCH.sub.2 CF.sub.3                                                                          H        OMe                                                      OCH.sub.2 CF.sub.3                                                                          Me       OMe                                                      OCH.sub.2 CF.sub.3                                                                          H        OCF.sub.2 H                                              OCH.sub.2 CF.sub.3                                                                          Me       OCF.sub.2 H                                              O(CH.sub.2).sub.2 Cl                                                                        H        Me                                                       O(CH.sub.2).sub.2 Cl                                                                        Me       Me                                                       O(CH.sub.2).sub.2 Cl                                                                        H        OMe                                                      O(CH.sub.2).sub.2 Cl                                                                        Me       OMe                                                      O(CH.sub.2).sub.2 Cl                                                                        H        OCF.sub.2 H                                              O(CH.sub.2).sub.2 Cl                                                                        Me       OCF.sub.2 H                                              S(O)Me       H        Me                                                       S(O)Me       Me       Me                                                       S(O)Me       H        OMe                                                      S(O)Me       Me       OMe                                                      S(O)Me       H        OCF.sub.2 H                                              S(O)Me       Me       OCF.sub.2 H                                              S(O)Et       H        Me                                                       S(O)Et       Me       Me                                                       S(O)Et       H        OMe                                                      S(O)Et       Me       OMe                                                      S(O)Et       H        OCF.sub.2 H                                              S(O)Et       Me       OCF.sub.2 H                                              S(O)-- -n-Pr H        Me                                                       S(O)-- -n-Pr Me       Me                                                       S(O)-- -n-Pr H        OMe                                                      S(O)-- -n-Pr Me       OMe                                                      S(O)-- -n-Pr H        OCF.sub.2 H                                              S(O)-- -n-Pr Me       OCF.sub.2 H                                              S(O)-- .sub.-i-Pr                                                                           H        Me                                                       S(O)-- .sub.-i-Pr                                                                           Me       Me                                                       S(O)-- .sub.-i-Pr                                                                           H        OMe                                                      S(O)-- .sub.-i-Pr                                                                           Me       Me                                                       S(O)-- .sub.-i-Pr                                                                           H        OCF.sub.2 H                                              S(O)-- .sub.-i-Pr                                                                           Me       OCF.sub.2 H                                              SO.sub.2 Me  H        Me                                                       SO.sub.2 Me  Me       Me                                                       SO.sub.2 Me  H        OMe                                                      SO.sub.2 Me  Me       OMe                                                      SO.sub.2 Me  H        OCF.sub.2 H                                              SO.sub.2 Me  Me       OCF.sub.2 H                                              SO.sub.2 Et  H        Me                                                       SO.sub.2 Et  Me       Me                                                       SO.sub.2 Et  H        OMe                                                      SO.sub.2 Et  Me       OMe                                                      SO.sub.2 Et  H        OCF.sub.2 H                                              SO.sub.2 Et  Me       OCF.sub.2 H                                              SO.sub.2 -- -n-Pr                                                                           H        Me                                                       SO.sub.2 -- -n-Pr                                                                           Me       Me                                                       SO.sub.2 -- -n-Pr                                                                           H        OMe                                                      SO.sub.2 -- -n-Pr                                                                           Me       OMe                                                      SO.sub.2 -- -n-Pr                                                                           H        OCF.sub.2 H                                              SO.sub.2 -- -n-Pr                                                                           Me       OCF.sub.2 H                                              SO.sub.2 -- .sub.-i-Pr                                                                      H        Me                                                       SO.sub.2 -- .sub.-i-Pr                                                                      Me       Me                                                       SO.sub.2 -- .sub.-i-Pr                                                                      H        OMe                                                      SO.sub.2 -- .sub.-i-Pr                                                                      Me       OMe                                                      SO.sub.2 -- .sub.-i-Pr                                                                      H        OCF.sub.2 H                                              SO.sub.2 -- .sub.-i-Pr                                                                      Me       OCF.sub.2 H                                              S--allyl     H        Me                                                       S--allyl     Me       Me                                                       S--allyl     H        OMe                                                      S--allyl     Me       OMe                                                      S--allyl     H        OCF.sub.2 H                                              S--allyl     Me       OCF.sub.2 H                                              S(O)allyl    H        Me                                                       S(O)allyl    Me       Me                                                       S(O)allYl    H        OMe                                                      S(O)allyl    Me       OMe                                                      S(O)allyl    H        OCF.sub.2 H                                              S(O)allyl    Me       OCF.sub.2 H                                              SO.sub.2 allyl                                                                              H        Me                                                       SO.sub.2 allyl                                                                              Me       Me                                                       SO.sub.2 allyl                                                                              H        OMe                                                      SO.sub.2 allyl                                                                              Me       OMe                                                      SO.sub.2 allyl                                                                              H        OCF.sub.2 H                                              SO.sub.2 allyl                                                                              Me       OCF.sub.2 H                                              S--propargyl H        Me                                                       S--propargyl Me       Me                                                       S--propargyl H        OMe                                                      S--propargyl Me       OMe                                                      S--propargyl H        OCF.sub.2 H                                              S--propargyl Me       OCF.sub.2 H                                              S(O)proparyl H        Me                                                       S(O)propargyl                                                                               Me       Me                                                       S(O)propargyl                                                                               H        OMe                                                      S(O)propargyl                                                                               Me       OMe                                                      S(O)propargyl                                                                               H        OCF.sub.2 H                                              S(O)propargyl                                                                               Me       OCF.sub.2 H                                              SO.sub.2 propargyl                                                                          H        Me                                                       SO.sub.2 propargyl                                                                          Me       Me                                                       SO.sub.2 propargyl                                                                          H        OMe                                                      SO.sub.2 propargyl                                                                          Me       OMe                                                      SO.sub.2 propargyl                                                                          H        OCF.sub.2 H                                              SO.sub.2 propargyl                                                                          Me       OCF.sub.2 H                                              ______________________________________                                    

                  TABLE IVa                                                        ______________________________________                                         R.sub.1 = i-Pr                                                                 R.sub.2         R       Y         m.p. (°C.)                            ______________________________________                                         CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       Me                                                     CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OMe                                                    CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       Me                                                     (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OMe                                                    (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            CH.sub.3                                                                               Me                                                     CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       Me                                                     CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       Me                                                     CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       OMe                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       Me                                                     (CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       OMe                                                    CH.sub.2 OCF.sub.2 H                                                                           H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                  CH.sub.3                                                                               OMe                                                    CH.sub.2 OCH.sub.2 CHF.sub.2                                                                   H       Me                                                     CH.sub.2 OCH.sub.2 CH.sub. 2 Br                                                                H       OMe                                                    CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                 H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CH.sub.2 I                                                                  H       Me                                                     CH.sub.2 OCF.sub.3                                                                             H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       Me                                                     CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OMe                                                    (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            CH.sub.3                                                                               OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       Me                                                     (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                    CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                            CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       Me                                                     CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       Me                                                     CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OMe                                                    (CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OMe                                                    CH(CH.sub.3)S(O).sub.2 CH.sub.3                                                                H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          CH.sub.3                                                                               Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                  H       OMe                                                    CH.sub.2 S(O).sub.2 CF.sub.2 H                                                                 H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 F                                                        H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CHF.sub.2                                                         H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 Br                                                       H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 I                                                        CH.sub.3                                                                               OMe                                                    CH.sub.2 S(O).sub.2 CF.sub.3                                                                   H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                H       OMe                                                    OCH.sub.2 OCH.sub.3                                                                            H       OCF.sub.2 H                                            OCH.sub.2 OCH.sub.3                                                                            H       Me                                                     OCH.sub.2 OCH.sub.3                                                                            H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OCF.sub. 2 H                                           O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           CH.sub.3                                                                               OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OMe                                                    OCH.sub.2 OCH.sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            H       Me                                                     CH.sub.2 SCF.sub.2 H                                                                           H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.2 F                                                                  H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CHF.sub.2                                                                   H       Me                                                     CH.sub.2 SCH.sub.2 CH.sub.2 Br                                                                 H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.2 Cl                                                                 H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CH.sub.2 I                                                                  CH.sub.3                                                                               Me                                                     CH.sub.2 SCF.sub.3                                                                             H       Me                                                     CH.sub.2 S(O)CH.sub.3                                                                          H       OMe                                                    CH.sub.2 S(O)CH.sub.3                                                                          H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.3                                                                          H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OMe                                                    (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       Me                                                     CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH.sub. 2 S(O)CH.sub.2 CH.sub.3                                                                H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 CH.sub.3                                                                               OMe                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         H       OMe                                                    CH(CH.sub.3)S(O)CH.sub.3                                                                       H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       Me                                                     CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       OMe                                                    CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                       H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                         H       OMe                                                    CH.sub.2 S(O)CF.sub.2 H                                                                        H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CH.sub.2 F                                                               CH.sub.3                                                                               OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CHF.sub.2                                                                H       Me                                                     CH.sub.2 S(O)CH.sub.2 CH.sub.2 Br                                                              H       OMe                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.2 I                                                               H       OCF.sub.2 H                                            CH.sub.2 S(O)CF.sub.3                                                                          H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OMe                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            OCH.sub.2 OCH.sub.2 CF.sub.3                                                                   H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                           H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                         H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                         H       Me                                                     O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                         H       OMe                                                    O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                          H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCF.sub.3                                                                    H       Me                                                     OCH.sub.2 SCH.sub.3                                                                            H       OMe                                                    OCH.sub.2 SCH.sub.3                                                                            H       OCF.sub.2 H                                            OCH.sub.2 SCH.sub.3                                                                            H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OMe                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.3                                                                    CH.sub.3                                                                               Me                                                     O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OMe                                                    O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       Me                                                     OCH.sub.2 SCH.sub.2 CH.sub.3                                                                   H       OMe                                                    OCH.sub.2 SCH.sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                           H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(CH.sub.2 ).sub.2 Cl                                                        H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                         CH.sub.3                                                                               OMe                                                    O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                          H       Me                                                     O(CH.sub.2).sub.2 SCF.sub.3                                                                    H       OMe                                                    OCH.sub.2 S(O)CH.sub.3                                                                         H       OCF.sub.2 H                                            OCH.sub.2 S(O)CH.sub.3                                                                         H       Me                                                     OCH.sub.2 S(O)CH.sub.3                                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                 H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                 H       Me                                                     O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                 H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        CH.sub.3                                                                               OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        H       Me                                                     OCH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                        H       OCF.sub.2 H                                            OCH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                H       Me                                                     O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                      H       OME                                                    O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Cl                                                      H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Br                                                      H       Me                                                     O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 I                                                       H       OMe                                                    O(CH.sub.2).sub.2 S(O)CF.sub.3                                                                 H       OCF.sub.2 H                                            OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       OMe                                                    OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 CH.sub.3                                                                               Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       OCF.sub.2 H                                            OCH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                         H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                 H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                               H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Cl                                               H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Br                                               H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 I                                                CH.sub.3                                                                               OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CF.sub.3                                                          H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                               H       OMe                                                    OCH.sub.2 S(O).sub.2 CF.sub.3                                                                  H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 CN                                                                           H       Me                                                     O(CH.sub.2).sub.2 CN                                                                           H       OMe                                                    O(CH.sub.2).sub.2 CN                                                                           H       OCF.sub.2 H                                            OCH.sub.2 CN    H       Me                                                     OCH.sub.2 CN    H       OMe                                                    OCH.sub.2 CN    H       OCF.sub.2 H                                            OCH.sub.2 CN    CH.sub.3                                                                               OCF.sub.2 H                                            OCH(CH.sub.3)CN H       Me                                                     O(CH.sub.2).sub.2 NH.sub.2                                                                     H       OMe                                                    O(CH.sub.2).sub.2 NH.sub.2                                                                     H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 NH.sub.2                                                                     H       Me                                                     O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       OMe                                                    O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       Me                                                     O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       OMe                                                    O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       Me                                                     SCH.sub.2 OCH.sub.3                                                                            H       OMe                                                    SCH.sub.2 OCH.sub.3                                                                            H       OCF.sub.2 H                                            SCH.sub.2 OCH.sub.3                                                                            H       Me                                                     SCH.sub.2 OCH.sub.2 CH.sub.3                                                                   H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub. 3                                                                   H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCH.sub.3                                                                    CH.sub.3                                                                               Me                                                     S(CH.sub.2).sub.2 OCH.sub.3                                                                    H       Me                                                     S(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                           H       Me                                                     SCH.sub.2 OCH.sub.2 CF.sub.3                                                                   H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                         H       Me                                                     S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                         H       OMe                                                    S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                          H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCF.sub.3                                                                    CH.sub.3                                                                               OMe                                                    SCH.sub.2 SCH.sub.3                                                                            H       Me                                                     SCH.sub.2 SCH.sub.3                                                                            H       OMe                                                    SCH.sub.2 SCH.sub.3                                                                            H       OCF.sub.2 H                                            SCH.sub.2 SCH.sub.2 CH.sub.3                                                                   H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OMe                                                    S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OMe                                                    SCH(CH.sub.3)SCH.sub.3                                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                           CH.sub.3                                                                               OCF.sub. 2 H                                           SCH.sub.2 SCH.sub.2 CF.sub.3                                                                   H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                         H       OMe                                                    S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                         H       Me                                                     S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                          H       OMe                                                    S(CH.sub.2).sub.2 SCF.sub.3                                                                    H       OCF.sub.2 H                                            SCH.sub.2 CN    H       Me                                                     SCH.sub.2 CN    H       OMe                                                    SCH.sub.2 CN    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CN                                                                           H       Me                                                     S(CH.sub.2).sub.2 CN                                                                           H       OMe                                                    S(CH.sub.2).sub.2 CN                                                                           H       OCF.sub.2 H                                            SCH(CH.sub.3)CN H       Me                                                     SCHF.sub.2      H       OMe                                                    SCHF.sub.2      H       OCF.sub.2 H                                            SCHF.sub.2      CH.sub.3                                                                               Me                                                     SCHF.sub.2      H       Me                                                     SCF.sub.3       H       OMe                                                    SCH.sub.2 CFH.sub.2                                                                            H       OCF.sub.2 H                                            SCH.sub.2 CF.sub.2 H                                                                           H       Me                                                     SCH.sub.2 CF.sub.3                                                                             H       OMe                                                    SCH.sub.2 CF.sub.3                                                                             H       OCF.sub.2 H                                            SCH.sub.2 CF.sub.3                                                                             H       Me                                                     SCH.sub.2 CF.sub.2 H                                                                           H       OMe                                                    S(CH.sub.2).sub.2 CFH.sub.2                                                                    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CClH.sub.2                                                                   CH.sub.3                                                                               OMe                                                    S(CH.sub.2).sub.2 CIH.sub.2                                                                    H       Me                                                     SCF.sub.2 CF.sub.3                                                                             H       OMe                                                    SCH(CH.sub.3)CF.sub.3                                                                          H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CCl.sub.3                                                                    H       Me                                                     S(O)CHF.sub.2   H       OMe                                                    S(O)CHF.sub.2   H       OCF.sub.2 H                                            S(O)CHF.sub.2   H       Me                                                     S(O)CF.sub.3    H       OMe                                                    S(O)CH.sub.2 CFH.sub.2                                                                         H       OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.2 H                                                                        CH.sub.3                                                                               OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.3                                                                          H       Me                                                     S(O)CH.sub.2 CF.sub.3                                                                          H       OMe                                                    S(O)CH.sub.2 CF.sub.3                                                                          H       OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.2 H                                                                        H       Me                                                     S(O)(CH.sub.2).sub.2 CFH.sub.2                                                                 H       OMe                                                    S(O)(CH.sub.2).sub.2 CClH.sub.2                                                                H       OCF.sub.2 H                                            S(O)(CH.sub.2).sub.2 CIH.sub.2                                                                 H       Me                                                     S(O)CF.sub.2 CF.sub.3                                                                          H       OMe                                                    S(O)CH(CH.sub.3)CF.sub.3                                                                       H       OCF.sub.2 H                                            S(O)(CH.sub.2).sub.2 CCl.sub.3                                                                 H       Me                                                     S(O).sub.2 CHF.sub.2                                                                           H       OMe                                                    S(O).sub.2 CHF.sub.2                                                                           H       OCF.sub.2 H                                            S(O).sub.2 CHF.sub.2                                                                           H       Me                                                     S(O).sub.2 CF.sub.3                                                                            H       OMe                                                    S(O).sub.2 CH.sub.2 CFH.sub.2                                                                  H       OCF.sub.2 H                                            S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                 CH.sub.3                                                                               Me                                                     S(O).sub.2 CH.sub.2 CF.sub.3                                                                   H       Me                                                     S(O).sub.2 CH.sub.2 CF.sub.3                                                                   H       OMe                                                    S(O).sub.2 CH.sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                            S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                 H       Me                                                     S(O).sub.2 (CH.sub.2).sub.2 CFH.sub.2                                                          H       OMe                                                    S(O).sub.2 (CH.sub.2).sub.2 CClH.sub.2                                                         H       OCF.sub.2 H                                            S(O).sub.2 (CH.sub.2).sub.2 CIH.sub.2                                                          H       Me                                                     S(O).sub.2 CF.sub.2 CF.sub.3                                                                   H       OMe                                                    S(O).sub.2 CH(CH.sub.3)CF.sub.3                                                                H       OCF.sub.2 H                                            S(O).sub.2 (CH.sub.2).sub.2 CCl.sub.3                                                          CH.sub.3                                                                               OMe                                                    S(O).sub.2 CH.sub.2 Cl                                                                         H       Me                                                     CH═CH.sub.2 H       OMe                                                    CH═CH.sub.2 H       OCF.sub.2 H                                            CH═CH.sub.2 H       Me                                                     CH.sub.2 CH═CH.sub.2                                                                       H       OMe                                                    CH.sub.2 CH═CH.sub.2                                                                       H       OCF.sub.2 H                                            CH.sub.2 CH═CH.sub.2                                                                       H       Me                                                     CH═CHCH.sub.3                                                                              H       OMe                                                    C(CH.sub.3)═CH.sub.2                                                                       H       OCF.sub.2 H                                            CH═CH.sub.2 CH.sub.3                                                                               OCF.sub.2 H                                            C.tbd.CH        H       Me                                                     C.tbd.CH        H       OMe                                                    C.tbd.CH        H       OCF.sub.2 H                                            CH.sub.2 C.tbd.CH                                                                              H       Me                                                     CH.sub.2 C.tbd.CH                                                                              H       OMe                                                    CH.sub.2 C.tbd.CH                                                                              H       OCF.sub.2 H                                            C.tbd.CCH.sub.3 H       Me                                                     C.tbd.CCH.sub.3 H       OMe                                                    C.tbd. CCH.sub.3                                                                               H       OCF.sub.2 H                                            NH.sub.2        H       Me                                                     NH.sub.2        H       OMe                                                    NH.sub.2        H       OCF.sub.2 H                                            NHCH.sub.3      H       Me                                                     NHCH.sub.3      H       OMe                                                    NHCH.sub.3      H       OCF.sub.2 H                                            NHCH.sub.3      CH.sub.3                                                                               Me                                                     N(CH.sub.3).sub.2                                                                              H       Me                                                     N(CH.sub.3).sub.2                                                                              H       OMe                                                    N(CH.sub.3).sub.2                                                                              H       OCF.sub.2 H                                            NHCH.sub.2 CH.sub.3                                                                            H       Me                                                     NHCH.sub.2 CH.sub.3                                                                            H       OMe                                                    NHCH.sub.2 CH.sub.3                                                                            H       OCF.sub.2 H                                            N(CH.sub.3)CH.sub.2 CH.sub.3                                                                   H       Me                                                     N(CH.sub.2 CH.sub.3).sub.2                                                                     H       OMe                                                    NHCH.sub.2 CF.sub.3                                                                            H       OCF.sub.2 H                                            NHCH.sub.2 CF.sub.3                                                                            CH.sub.3                                                                               OMe                                                    NHCH.sub.2 CF.sub.3                                                                            H       Me                                                     NHCH.sub.2 CF.sub.3                                                                            H       OMe                                                    N(CH.sub.3)CH.sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                            N(CH.sub.3)CH.sub.2 CHF.sub.2                                                                  H       Me                                                     N(CH.sub.3)(CH.sub.2).sub.2 F                                                                  H       OMe                                                    N(CH.sub.3)(CH.sub.2).sub.2 Cl                                                                 H       OCF.sub.2 H                                            N(CH.sub.3)(CH.sub.2).sub.2 I                                                                  H       Me                                                     N(CH.sub.3)(CH.sub.2).sub.2 Br                                                                 H       OMe                                                    NHCF.sub.3      CH.sub.3                                                                               OCF.sub.2 H                                            NHCF.sub.3      H       Me                                                     NH(CH.sub.2).sub.2 F                                                                           H       OMe                                                    N(CH.sub.3)CF.sub.2 H                                                                          H       OCF.sub.2 H                                            NHCF.sub.2 H    H       Me                                                     ______________________________________                                    

                  TABLE Va                                                         ______________________________________                                         R.sub.1 = CH.sub.2 CH═CH.sub.2                                             R.sub.2          R       Y         m.p. (°C.)                           ______________________________________                                         Me               H       Me                                                    Me               Me      Me                                                    Me               H       OMe                                                   Me               Me      OMe                                                   Me               H       OCF.sub.2 H                                           Me               Me      OCF.sub.2 H                                           Et               H       Me                                                    Et               Me      Me                                                    Et               H       OMe                                                   Et               Me      OMe                                                   Et               H       OCF.sub.2 H                                           Et               Me      OCF.sub.2 H                                           Pr               H       Me                                                    Pr               Me      Me                                                    Pr               H       OMe                                                   Pr               Me      OMe                                                   Pr               H       OCF.sub.2 H                                           Pr               Me      OCF.sub.2 H                                            .sub.-i-Pr      H       Me                                                     .sub.-i-Pr      Me      Me                                                     .sub.-i-Pr      H       OMe                                                    .sub.-i-Pr      Me      OMe                                                    .sub.-i-Pr      H       OCF.sub.2 H                                            .sub.-i-Pr      Me      OCF.sub.2 H                                           cyclo-Pr         H       Me                                                    cyclo-Pr         Me      Me                                                    cyclo-Pr         H       OMe                                                   cyclo-Pr         Me      OMe                                                   cyclo-Pr         H       OCF.sub.2 H                                           cyclo-Pr         Me      OCF.sub.2 H                                           OMe              H       Me                                                    OMe              Me      Me                                                    OMe              H       OMe                                                   OMe              Me      OMe                                                   OMe              H       OCF.sub.2 H                                           OMe              Me      OCF.sub.2 H                                           OEt              H       Me                                                    OEt              Me      Me                                                    OEt              H       OMe                                                   OEt              Me      OMe                                                   OEt              H       OCF.sub.2 H                                           OEt              Me      OCF.sub.2 H                                           O-- -n-Pr        H       Me                                                    O-- -n-Pr        Me      Me                                                    O-- -n-Pr        H       OMe                                                   O-- -n-Pr        Me      OMe                                                   O-- -n-Pr        H       OCF.sub.2 H                                           O-- -n-Pr        Me      OCF.sub.2 H                                           O-- .sub.-i-Pr   H       Me                                                    O-- .sub.-i-Pr   Me      Me                                                    O-- .sub.-i-Pr   H       OMe                                                   O-- .sub.-i-Pr   Me      OMe                                                   O-- .sub.-i-Pr   H       OCF.sub.2 H                                           O-- .sub.-i-Pr   Me      OCF.sub.2 H                                           SMe              H       Me        133-137                                     SMe              Me      Me                                                    SMe              H       OMe       126-131                                     SMe              Me      OMe                                                   SMe              H       OCF.sub.2 H                                           SMe              Me      OCF.sub.2 H                                           SEt              H       Me                                                    SEt              Me      Me                                                    SEt              H       OMe                                                   SEt              Me      OMe                                                   SEt              H       OCF.sub.2 H                                           SEt              Me      OCF.sub.2 H                                           S-- -n-Pr        H       Me                                                    S-- -n-Pr        Me      Me                                                    S-- -n-Pr        H       OMe                                                   S--  -n-Pr       Me      OMe                                                   S-- -n-Pr        H       OCF.sub.2 H                                           S-- -n-Pr        Me      OCF.sub.2 H                                           S-- .sub.-i-Pr   H       Me                                                    S-- .sub.-i-Pr   Me      Me                                                    S-- .sub.-i-Pr   H       OMe                                                   S-- .sub.-i-Pr   Me      OMe                                                   S-- .sub.-i-Pr   H       OCF.sub.2 H                                           S-- .sub.-i-Pr   Me      OCF.sub.2 H                                           O--allyl         H       Me                                                    O--allyl         Me      Me                                                    O--allyl         H       OMe                                                   O--allyl         Me      OMe                                                   O--allyl         H       OCF.sub.2 H                                           O--allyl         Me      OCF.sub.2 H                                           O--propargyl     H       Me                                                    O--propargyl     Me      Me                                                    O--propargyl     H       OMe                                                   O--propargyl     Me      OMe                                                   O--propargyl     H       OCF.sub.2 H                                           O--propargyl     Me      OCF.sub.2 H                                           CH.sub.2 F       H       Me                                                    CH.sub.2 F       Me      Me                                                    CH.sub.2 F       H       OMe                                                   CH.sub.2 F       Me      OMe                                                   CH.sub.2 F       H       OCF.sub.2 H                                           CH.sub.2 F       Me      OCF.sub.2 H                                           CHF.sub.2        H       Me                                                    CHF.sub.2        Me      Me                                                    CHF.sub.2        H       OMe                                                   CHF.sub.2        Me      OMe                                                   CHF.sub.2        H       OCF.sub.2 H                                           CHF.sub.2        Me      OCF.sub. 2 H                                          CF.sub.3         H       Me                                                    CF.sub.3         Me      Me                                                    CF.sub.3         H       OMe       87-93                                       CF.sub.3         Me      OMe                                                   CF.sub.3         H       OCF.sub.2 H                                           CF.sub.3         Me      OCF.sub.2 H                                           CH.sub.2 Cl      H       Me                                                    CH.sub.2 Cl      Me      Me                                                    CH.sub.2 Cl      H       OMe                                                   CH.sub.2 Cl      Me      OMe                                                   CH.sub.2 Cl      H       OCF.sub.2 H                                           CH.sub.2 Cl      Me      OCF.sub.2 H                                           CHCl.sub.2       H       Me                                                    CHCl.sub.2       Me      Me                                                    CHCl.sub.2       H       OMe                                                   CHCl.sub.2       Me      OMe                                                   CHCl.sub.2       H       OCF.sub.2 H                                           CHCl.sub.2       Me      OCF.sub.2 H                                           CCl.sub.3        H       Me                                                    CCl.sub.3        Me      Me                                                    CCl.sub.3        H       OMe                                                   CCl.sub.3        Me      OMe                                                   CCl.sub.3        H       OCF.sub.2 H                                           CCl.sub.3        Me      OCF.sub.2 H                                           CHFCH.sub.3      H       Me                                                    CHFCH.sub.3      Me      Me                                                    CHFCH.sub.3      H       OMe                                                   CHFCH.sub.3      Me      OMe                                                   CHFCH.sub.3      H       OCF.sub.2 H                                           CHFCH.sub.3      Me      OCF.sub.2 H                                           CF.sub.2 CH.sub.3                                                                               H       Me                                                    CF.sub.2 CH.sub.3                                                                               Me      Me                                                    CF.sub.2 CH.sub.3                                                                               H       OMe                                                   CF.sub.2 CH.sub.3                                                                               Me      OMe                                                   CF.sub.2 CH.sub.3                                                                               H       OCF.sub.2 H                                           CF.sub.2 CH.sub.3                                                                               Me      OCF.sub.2 H                                           CH.sub.2 CH.sub.2 F                                                                             H       Me                                                    CH.sub.2 CH.sub. 2 F                                                                            Me      Me                                                    CH.sub.2 CH.sub.2 F                                                                             H       OMe                                                   CH.sub.2 CH.sub.2 F                                                                             Me      OMe                                                   CH.sub.2 CH.sub.2 F                                                                             H       OCF.sub.2 H                                           CH.sub.2 CH.sub.2 F                                                                             Me      OCF.sub.2 H                                           CH.sub.2 CHF.sub.2                                                                              H       Me                                                    CH.sub.2 CHF.sub.2                                                                              Me      Me                                                    CH.sub.2 CHF.sub.2                                                                              H       OMe                                                   CH.sub.2 CHF.sub.2                                                                              Me      OMe                                                   CH.sub.2 CHF.sub.2                                                                              H       OCF.sub.2 H                                           CH.sub.2 CHF.sub.2                                                                              Me      OCF.sub.2 H                                           CH.sub.2 CF.sub.3                                                                               H       Me                                                    CH.sub.2 CF.sub.3                                                                               Me      Me                                                    CH.sub.2 CF.sub.3                                                                               H       OMe                                                   CH.sub.2 CF.sub.3                                                                               Me      OMe                                                   CH.sub.2 CF.sub.3                                                                               H       OCF.sub.2 H                                           CH.sub.2 CF.sub.3                                                                               Me      OCF.sub.2 H                                           CHClCH.sub.3     H       Me                                                    CHClCH.sub.3     Me      Me                                                    CHClCH.sub.3     H       OMe                                                   CHClCH.sub.3     Me      OMe                                                   CHClCH.sub.3     H       OCF.sub.2 H                                           CHClCH.sub.3     Me      OCF.sub.2 H                                           CH.sub.2 OCH.sub.3                                                                              H       Me                                                    CH.sub.2 OCH.sub.3                                                                              Me      Me                                                    CH.sub.2 OCH.sub.3                                                                              H       OMe                                                   CH.sub.2 OCH.sub.3                                                                              Me      OMe                                                   CH.sub.2 OCH.sub.3                                                                              H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.3                                                                              Me      OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.3                                                                      H       Me                                                    (CH.sub.2).sub.2 OCH.sub.3                                                                      Me      Me                                                    (CH.sub.2).sub.2 OCH.sub.3                                                                      H       OMe                                                   (CH.sub.2).sub.2 OCH.sub.3                                                                      Me      OMe                                                   (CH.sub.2).sub.2 OCH.sub.3                                                                      H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.3                                                                      Me      OCF.sub.2 H                                           CH(OCH.sub.3)CH.sub.3                                                                           H       Me                                                    CH(OCH.sub.3)CH.sub.3                                                                           Me      Me                                                    CH(OCH.sub.3)CH.sub.3                                                                           H       OMe                                                   CH(OCH.sub.3)CH.sub.3                                                                           Me      OMe                                                   CH(OCH.sub.3)CH.sub.3                                                                           H       OCF.sub.2 H                                           CH(OCH.sub.3)CH.sub.3                                                                           Me      OCF.sub.2 H                                           CH.sub.2 SCH.sub.3                                                                              H       Me                                                    CH.sub.2 SCH.sub.3                                                                              Me      Me                                                    CH.sub.2 SCH.sub.3                                                                              H       OMe                                                   CH.sub.2 SCH.sub.3                                                                              Me      OMe                                                   CH.sub.2 SCH.sub.3                                                                              H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.3                                                                              Me      OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.3                                                                      H       Me                                                    (CH.sub.2).sub.2 SCH.sub.3                                                                      Me      Me                                                    (CH.sub.2).sub.2 SCH.sub.3                                                                      H       OMe                                                   (CH.sub.2).sub.2 SCH.sub.3                                                                      Me      OMe                                                   (CH.sub.2).sub.2 SCH.sub.3                                                                      H       OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.3                                                                      Me      OCF.sub.2 H                                           CH(SCH.sub.3)CH.sub.3                                                                           H       Me                                                    CH(SCH.sub.3)CH.sub.3                                                                           Me      Me                                                    CH(SCH.sub.3)CH.sub.3                                                                           H       OMe                                                   CH(SCH.sub.3)CH.sub.3                                                                           Me      OMe                                                   CH(SCH.sub.3)CH.sub.3                                                                           H       OCF.sub.2 H                                           CH(SCH.sub.3)CH.sub.3                                                                           Me      OCF.sub.2 H                                           OCF.sub.2 H      H       Me                                                    OCF.sub.2 H      Me      Me                                                    OCF.sub.2 H      H       OMe                                                   OCF.sub.2 H      Me      OMe                                                   OCF.sub.2 H      H       OCF.sub.2 H                                           OCF.sub.2 H      Me      OCF.sub.2 H                                           OCH.sub.2 CH.sub.2 F                                                                            H       Me                                                    OCH.sub.2 CH.sub.2 F                                                                            Me      Me                                                    OCH.sub.2 CH.sub.2 F                                                                            H       OMe                                                   OCH.sub.2 CH.sub.2 F                                                                            Me      OMe                                                   OCH.sub.2 CH.sub.2 F                                                                            H       OCF.sub.2 H                                           OCH.sub.2 CH.sub.2 F                                                                            Me      OCF.sub.2 H                                           OCH.sub.2 CHF.sub.2                                                                             H       Me                                                    OCH.sub.2 CHF.sub.2                                                                             Me      Me                                                    OCH.sub.2 CHF.sub.2                                                                             H       OMe                                                   OCH.sub.2 CHF.sub.2                                                                             Me      OMe                                                   OCH.sub.2 CHF.sub.2                                                                             H       OCF.sub.2 H                                           OCH.sub.2 CHF.sub.2                                                                             Me      OCF.sub.2 H                                           OCH.sub.2 CF.sub.3                                                                              H       Me                                                    OCH.sub.2 CF.sub.3                                                                              Me      Me                                                    OCH.sub.2 CF.sub.3                                                                              H       OMe                                                   OCH.sub.2 CF.sub.3                                                                              Me      OMe                                                   OCH.sub.2 CF.sub.3                                                                              H       OCF.sub.2 H                                           OCH.sub.2 CF.sub.3                                                                              Me      OCF.sub.2 H                                           O(CH.sub.2).sub.2 Cl                                                                            H       Me                                                    O(CH.sub.2).sub.2 Cl                                                                            Me      Me                                                    O(CH.sub.2).sub.2 Cl                                                                            H       OMe                                                   O(CH.sub.2).sub.2 Cl                                                                            Me      OMe                                                   O(CH.sub.2).sub.2 Cl                                                                            H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 Cl                                                                            Me      OCF.sub.2 H                                           S(O)Me           H       Me                                                    S(O)Me           Me      Me                                                    S(O)Me           H       OMe                                                   S(O)Me           Me      OMe                                                   S(O)Me           H       OCF.sub.2 H                                           S(O)Me           Me      OCF.sub.2 H                                           S(O)Et           H       Me                                                    S(O)Et           Me      Me                                                    S(O)Et           H       OMe                                                   S(O)Et           Me      OMe                                                   S(O)Et           H       OCF.sub.2 H                                           S(O)Et           Me      OCF.sub.2 H                                           S(O)-- -n-Pr     H       Me                                                    S(O)-- -n-Pr     Me      Me                                                    S(O)-- -n-Pr     H       OMe                                                   S(O)-- -n-Pr     Me      OMe                                                   S(O)-- -n-Pr     H       OCF.sub.2 H                                           S(O)-- -n-Pr     Me      OCF.sub.2 H                                           S(O)-- .sub.-i-Pr                                                                               H       Me                                                    S(O)-- .sub.-i-Pr                                                                               Me      Me                                                    S(O)-- .sub.-i-Pr                                                                               H       OMe                                                   S(O)-- .sub.-i-Pr                                                                               Me      Me                                                    S(O)-- .sub.-i-Pr                                                                               H       OCF.sub.2 H                                           S(O)-- .sub.-i-Pr                                                                               Me      OCF.sub.2 H                                           SO.sub.2 Me      H       Me                                                    SO.sub.2 Me      Me      Me                                                    SO.sub.2 Me      H       OMe                                                   SO.sub.2 Me      Me      OMe                                                   SO.sub.2 Me      H       OCF.sub.2 H                                           SO.sub.2 Me      Me      OCF.sub. 2 H                                          SO.sub.2 Et      H       Me                                                    SO.sub.2 Et      Me      Me                                                    SO.sub.2 Et      H       OMe                                                   SO.sub.2 Et      Me      OMe                                                   SO.sub.2 Et      H       OCF.sub.2 H                                           SO.sub.2 Et      Me      OCF.sub.2 H                                           SO.sub.2 -- -n-Pr                                                                               H       Me                                                    SO.sub.2 -- -n-Pr                                                                               Me      Me                                                    SO.sub.2 -- -n-Pr                                                                               H       OMe                                                   SO.sub.2 -- -n-Pr                                                                               Me      OMe                                                   SO.sub.2 -- -n-Pr                                                                               H       OCF.sub.2 H                                           SO.sub.2 -- -n-Pr                                                                               Me      OCF.sub.2 H                                           SO.sub.2 -- .sub.-i-Pr                                                                          H       Me                                                    SO.sub.2 -- .sub.-i-Pr                                                                          Me      Me                                                    SO.sub.2 -- .sub.-i-Pr                                                                          H       OMe                                                   SO.sub.2 -- .sub.-i-Pr                                                                          Me      OMe                                                   SO.sub.2 -- .sub.-i-Pr                                                                          H       OCF.sub.2 H                                           SO.sub.2 -- .sub.-i-Pr                                                                          Me      OCF.sub.2 H                                           S--allyl         H       Me                                                    S--allyl         Me      Me                                                    S--allyl         H       OMe                                                   S--allyl         Me      OMe                                                   S--allyl         H       OCF.sub.2 H                                           S--allyl         Me      OCF.sub.2 H                                           S(O)allyl        H       Me                                                    S(O)allyl        Me      Me                                                    S(O)allyl        H       OMe                                                   S(O)allyl        Me      OMe                                                   S(O)allyl        H       OCF.sub.2 H                                           S(O)allyl        Me      OCF.sub.2 H                                           SO.sub.2 allyl   H       Me                                                    SO.sub.2 allyl   Me      Me                                                    SO.sub.2 allyl   H       OMe                                                   SO.sub.2 allyl   Me      OMe                                                   SO.sub.2 allyl   H       OCF.sub.2 H                                           SO.sub.2 allyl   Me      OCF.sub.2 H                                           S-propargyl      H       Me                                                    S-propargyl      Me      Me                                                    S-propargyl      H       OMe                                                   S-propargyl      Me      OMe                                                   S-propargyl      H       OCF.sub.2 H                                           S-propargyl      Me      OCF.sub.2 H                                           S(O)propargyl    H       Me                                                    S(O)propargyl    Me      Me                                                    S(O)propargyl    H       OMe                                                   S(O)propargyl    Me      OMe                                                   S(O)propargyl    H       OCF.sub.2 H                                           S(O)propargyl    Me      OCF.sub.2 H                                           SO.sub.2 propargyl                                                                              H       Me                                                    SO.sub.2 propargyl                                                                              Me      Me                                                    SO.sub.2 propargyl                                                                              H       OMe                                                   SO.sub.2 propargyl                                                                              Me      OMe                                                   SO.sub.2 propargyl                                                                              H       OCF.sub.2 H                                           SO.sub.2 propargyl                                                                              Me      OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       Me                                                    CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       OMe                                                   CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       Me                                                    (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       OMe                                                   (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             CH.sub.3                                                                               Me                                                    CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                  H       Me                                                    CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CF.sub.3                                                                     H       Me                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                     H       OMe                                                   CH.sub.2 OCH.sub.2 CF.sub.3                                                                     H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                           H       Me                                                    (CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                             H       OMe                                                   CH.sub.2 OCF.sub.2 H                                                                            H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                   CH.sub.3                                                                               OMe                                                   CH.sub.2 OCH.sub.2 CHF.sub.2                                                                    H       Me                                                    CH.sub.2 OCH.sub.2 CH.sub.2 Br                                                                  H       OMe                                                   CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                  H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.2 I                                                                   H       Me                                                    CH.sub.2 OCF.sub.3                                                                              H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       Me                                                    CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       OMe                                                   (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             H       OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             CH.sub.3                                                                               OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             H       Me                                                    (CH.sub.2).sub. 2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                   CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       Me                                                    CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       Me                                                    CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       OMe                                                   (CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                           H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                   H       OMe                                                   CH(CH.sub.3)S(O).sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           CH.sub.3                                                                               Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                 H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                   H       OMe                                                   CH.sub.2 S(O).sub.2 CF.sub.2 H                                                                  H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 F                                                         H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CHF.sub.2                                                          H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 Br                                                        H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 I                                                         CH.sub.3                                                                               OMe                                                   CH.sub.2 S(O).sub.2 CF.sub.3                                                                    H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                 H       OMe                                                   OCH.sub.2 OCH.sub.3                                                                             H       OCF.sub.2 H                                           OCH.sub.2 OCH.sub.3                                                                             H       Me                                                    OCH.sub.2 OCH.sub.3                                                                             H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       Me                                                    O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            CH.sub.3                                                                               OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       Me                                                    O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OMe                                                   OCH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                             H       Me                                                    CH.sub.2 SCF.sub.2 H                                                                            H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.2 F                                                                   H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CHF.sub.2                                                                    H       Me                                                    CH.sub.2 SCH.sub.2 CH.sub.2 Br                                                                  H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.2 Cl                                                                  H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CH.sub.2 I                                                                   CH.sub.3                                                                               Me                                                    CH.sub.2 SCF.sub.3                                                                              H       Me                                                    CH.sub.2 S(O)CH.sub.3                                                                           H       OMe                                                   CH.sub.2 S(O)CH.sub.3                                                                           H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.3                                                                           H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       OMe                                                   (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       Me                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  CH.sub.3                                                                               OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                          H       OMe                                                   CH(CH.sub.3)S(O)CH.sub.3                                                                        H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                  H       Me                                                    CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                  H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                  H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                        H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                          H       OMe                                                   CH.sub. 2 S(O)CF.sub.2 H                                                                        H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CH.sub.2 F                                                                CH.sub.3                                                                               OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CHF.sub.2                                                                 H       Me                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.2 Br                                                               H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.2 I                                                                H       OCF.sub.2 H                                           CH.sub.2 S(O)CF.sub.3                                                                           H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       OMe                                                   (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           OCH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       Me                                                    O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                          H       Me                                                    O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                          H       OMe                                                   O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                           H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCF.sub.3                                                                     H       Me                                                    OCH.sub.2 SCH.sub.3                                                                             H       OMe                                                   OCH.sub.2 SCH.sub.3                                                                             H       OCF.sub.2 H                                           OCH.sub.2 SCH.sub.3                                                                             H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OMe                                                   O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 SCH.sub.3                                                                     CH.sub.3                                                                               Me                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                   O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       Me                                                    OCH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OMe                                                   OCH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OMe                                                   O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                          H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                          CH.sub.3                                                                               OMe                                                   O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                           H       Me                                                    O(CH.sub.2).sub.2 SCF.sub.3                                                                     H       OMe                                                   OCH.sub.2 S(O)CH.sub.3                                                                          H       OCF.sub.2 H                                           OCH.sub.2 S(O)CH.sub.3                                                                          H       Me                                                    OCH.sub.2 S(O)CH.sub.3                                                                          H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       Me                                                    O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         CH.sub.3                                                                               OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         H       Me                                                    OCH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                         H       OCF.sub.2 H                                           OCH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       Me                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                       H       OMe                                                   O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Cl                                                       H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Br                                                       H       Me                                                    O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 I                                                        H       OMe                                                   O(CH.sub.2).sub.2 S(O)CF.sub.3                                                                  H       OCF.sub.2 H                                           OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OMe                                                   OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  CH.sub.3                                                                               Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OCF.sub.2 H                                           OCH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                  H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Cl                                                H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Br                                                H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 I                                                 CH.sub.3                                                                               OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CF.sub.3                                                           H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                H       OMe                                                   OCH.sub.2 S(O).sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 CN                                                                            H       Me                                                    O(CH.sub.2).sub.2 CN                                                                            H       OMe                                                   O(CH.sub.2).sub.2 CN                                                                            H       OCF.sub.2 H                                           OCH.sub.2 CN     H       Me                                                    OCH.sub.2 CN     H       OMe                                                   OCH.sub.2 CN     H       OCF.sub.2 H                                           OCH.sub.2 CN     CH.sub.3                                                                               OCF.sub.2 H                                           OCH(CH.sub.3)CN  H       Me                                                    O(CH.sub.2).sub.2 NH.sub.2                                                                      H       OMe                                                   O(CH.sub. 2).sub.2 NH.sub.2                                                                     H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 NH.sub.2                                                                      H       Me                                                    O(CH.sub.2).sub.2 NHCH.sub.3                                                                    H       OMe                                                   O(CH.sub.2).sub.2 NHCH.sub.3                                                                    H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 NHCH.sub.3                                                                    H       Me                                                    O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       OMe                                                   O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       Me                                                    SCH.sub.2 OCH.sub.3                                                                             H       OMe                                                   SCH.sub.2 OCH.sub.3                                                                             H       OCF.sub.2 H                                           SCH.sub.2 OCH.sub.3                                                                             H       Me                                                    SCH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OMe                                                   S(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 OCH.sub.3                                                                     CH.sub.3                                                                               Me                                                    S(CH.sub.2).sub.2 OCH.sub.3                                                                     H       Me                                                    S(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OMe                                                   S(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       Me                                                    SCH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       OMe                                                   S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                          H       Me                                                    S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                          H       OMe                                                   S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                           H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 OCF.sub.3                                                                     CH.sub.3                                                                               OMe                                                   SCH.sub.2 SCH.sub.3                                                                             H       Me                                                    SCH.sub.2 SCH.sub.3                                                                             H       OMe                                                   SCH.sub.2 SCH.sub.3                                                                             H       OCF.sub.2 H                                           SCH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OMe                                                   S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                   SCH(CH.sub.3)SCH.sub.3                                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            CH.sub.3                                                                               OCF.sub.2 H                                           SCH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OMe                                                   S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                          H       Me                                                    S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                           H       OMe                                                   S(CH.sub.2).sub.2 SCF.sub.3                                                                     H       OCF.sub.2 H                                           SCH.sub.2 CN     H       Me                                                    SCH.sub.2 CN     H       OMe                                                   SCH.sub.2 CN     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CN                                                                            H       Me                                                    S(CH.sub.2 ).sub.2 CN                                                                           H       OMe                                                   S(CH.sub.2).sub.2 CN                                                                            H       OCF.sub.2 H                                           SCH(CH.sub.3)CN  H       Me                                                    SCHF.sub.2       H       OMe                                                   SCHF.sub.2       H       OCF.sub.2 H                                           SCHF.sub.2       CH.sub.3                                                                               Me                                                    SCHF.sub.2       H       Me                                                    SCF.sub.3        H       OMe                                                   SCH.sub.2 CFH.sub.2                                                                             H       OCF.sub.2 H                                           SCH.sub.2 CF.sub.2 H                                                                            H       Me                                                    SCH.sub.2 CF.sub.3                                                                              H       OMe                                                   SCH.sub.2 CF.sub.3                                                                              H       OCF.sub.2 H                                           SCH.sub.2 CF.sub.3                                                                              H       Me                                                    SCH.sub.2 CF.sub.2 H                                                                            H       OMe                                                   S(CH.sub.2).sub.2 CFH.sub.2                                                                     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CClH.sub.2                                                                    CH.sub.3                                                                               OMe                                                   S(CH.sub.2).sub.2 CIH.sub.2                                                                     H       Me                                                    SCF.sub.2 CF.sub.3                                                                              H       OMe                                                   SCH(CH.sub.3)CF.sub.3                                                                           H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CCl.sub.3                                                                     H       Me                                                    S(O)CHF.sub.2    H       OMe                                                   S(O)CHF.sub.2    H       OCF.sub.2 H                                           S(O)CHF.sub.2    H       Me                                                    S(O)CF.sub.3     H       OMe                                                   S(O)CH.sub.2 CFH.sub.2                                                                          H       OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.2 H                                                                         CH.sub.3                                                                               OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.3                                                                           H       Me                                                    S(O)CH.sub.2 CF.sub.3                                                                           H       OMe                                                   S(O)CH.sub.2 CF.sub.3                                                                           H       OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.2 H                                                                         H       Me                                                    S(O)(CH.sub.2).sub.2 CFH.sub.2                                                                  H       OMe                                                   S(O)(CH.sub.2).sub.2 CClH.sub.2                                                                 H       OCF.sub.2 H                                           S(O)(CH.sub.2).sub.2 CIH.sub.2                                                                  H       Me                                                    S(O)CF.sub.2 CF.sub.3                                                                           H       OMe                                                   S(O)CH(CH.sub.3)CF.sub.3                                                                        H       OCF.sub.2 H                                           S(O)(CH.sub.2).sub.2 CCl.sub.3                                                                  H       Me                                                    S(O).sub.2 CHF.sub.2                                                                            H       OMe                                                   S(O).sub.2 CHF.sub.2                                                                            H       OCF.sub.2 H                                           S(O).sub.2 CHF.sub.2                                                                            H       Me                                                    S(O).sub.2 CF.sub.3                                                                             H       OMe                                                   S(O).sub.2 CH.sub.2 CFH.sub.2                                                                   H       OCF.sub.2 H                                           S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                  CH.sub.3                                                                               Me                                                    S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       Me                                                    S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       OMe                                                   S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                  H       Me                                                    S(O).sub.2 (CH.sub.2).sub.2 CFH.sub.2                                                           H       OMe                                                   S(O).sub.2 (CH.sub.2).sub.2 CClH.sub.2                                                          H       OCF.sub.2 H                                           S(O).sub.2 (CH.sub.2).sub.2 CIH.sub.2                                                           H       Me                                                    S(O).sub.2 CF.sub.2 CF.sub.3                                                                    H       OMe                                                   S(O).sub.2 CH(CH.sub.3)CF.sub.3                                                                 H       OCF.sub.2 H                                           S(O).sub.2 (CH.sub.2).sub.2 CCl.sub.3                                                           CH.sub.3                                                                               OMe                                                   S(O).sub.2 CH.sub.2 Cl                                                                          H       Me                                                    CH═CH.sub.2  H       OMe                                                   CH═CH.sub. 2 H       OCF.sub.2 H                                           CH═CH.sub.2  H       Me                                                    CH.sub.2 CH═CH.sub.2                                                                        H       OMe                                                   CH.sub.2 CH═CH.sub.2                                                                        H       OCF.sub.2 H                                           CH.sub.2 CH═CH.sub.2                                                                        H       Me                                                    CH═CHCH.sub.3                                                                               H       OMe                                                   C(CH.sub.3)═CH.sub.2                                                                        H       OCF.sub.2 H                                           CH═CH.sub.2  CH.sub.3                                                                               OCF.sub.2 H                                           C.tbd.CH         H       Me                                                    C.tbd.CH         H       OMe                                                   C.tbd.CH         H       OCF.sub.2 H                                           CH.sub.2 C.tbd.CH                                                                               H       Me                                                    CH.sub.2 C.tbd.CH                                                                               H       OMe                                                   CH.sub.2 C.tbd.CH                                                                               H       OCF.sub.2 H                                           C.tbd.CCH.sub.3  H       Me                                                    C.tbd.CCH.sub.3  H       OMe                                                   C.tbd.CCH.sub.3  H       OCF.sub.2 H                                           NH.sub.2         H       Me                                                    NH.sub.2         H       OMe                                                   NH.sub.2         H       OCF.sub.2 H                                           NHCH.sub.3       H       Me                                                    NHCH.sub.3       H       OMe                                                   NHCH.sub.3       H       OCF.sub.2 H                                           NHCH.sub.3       CH.sub.3                                                                               Me                                                    N(CH.sub.3).sub.2                                                                               H       Me                                                    N(CH.sub.3).sub.2                                                                               H       OMe                                                   N(CH.sub.3).sub.2                                                                               H       OCF.sub.2 H                                           NHCH.sub.2 CH.sub.3                                                                             H       Me                                                    NHCH.sub.2 CH.sub.3                                                                             H       OMe                                                   NHCH.sub.2 CH.sub.3                                                                             H       OCF.sub.2 H                                           N(CH.sub.3)CH.sub.2 CH.sub.3                                                                    H       Me                                                    N(CH.sub.2 CH.sub.3).sub.2                                                                      H       OMe                                                   NHCH.sub.2 CF.sub.3                                                                             H       OCF.sub.2 H                                           NHCH.sub.2 CF.sub.3                                                                             CH.sub.3                                                                               OMe                                                   NHCH.sub.2 CF.sub.3                                                                             H       Me                                                    NHCH.sub.2 CF.sub.3                                                                             H       OMe                                                   N(CH.sub.3)CH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           N(CH.sub.3)CH.sub.2 CHF.sub.2                                                                   H       Me                                                    N(CH.sub.3)(CH.sub.2).sub.2 F                                                                   H       OMe                                                   N(CH.sub.3)(CH.sub.2).sub.2 Cl                                                                  H       OCF.sub.2 H                                           N(CH.sub.3)(CH.sub.2).sub.2 I                                                                   H       Me                                                    N(CH.sub.3)(CH.sub.2).sub.2 Br                                                                  H       OMe                                                   NHCF.sub.3       CH.sub.3                                                                               OCF.sub.2 H                                           NHCF.sub.3       H       Me                                                    NH(CH.sub.2).sub.2 F                                                                            H       OMe                                                   N(CH.sub.3)CF.sub.2 H                                                                           H       OCF.sub.2 H                                           NHCF.sub.2 H     H       Me                                                    ______________________________________                                    

                  TABLE VIa                                                        ______________________________________                                         R.sub.1 = CH.sub.2 CH.sub.2 OCH.sub.3                                          R.sub.2          R       Y         m.p. (°C.)                           ______________________________________                                         Me               H       Me                                                    Me               Me      Me                                                    Me               H       OMe                                                   Me               Me      OMe                                                   Me               H       OCF.sub.2 H                                           Me               Me      OCF.sub.2 H                                           Et               H       Me                                                    Et               Me      Me                                                    Et               H       OMe                                                   Et               Me      OMe                                                   Et               H       OCF.sub.2 H                                           Et               Me      OCF.sub.2 H                                           Pr               H       Me                                                    Pr               Me      Me                                                    Pr               H       OMe                                                   Pr               Me      OMe                                                   Pr               H       OCF.sub.2 H                                           Pr               Me      OCF.sub.2 H                                            .sub.-i-Pr      H       Me                                                     .sub.-i-Pr      Me      Me                                                     .sub.-i-Pr      H       OMe                                                    .sub.-i-Pr      Me      OMe                                                    .sub.-i-Pr      H       OCF.sub.2 H                                            .sub.-i-Pr      Me      OCF.sub.2 H                                           cyclo-Pr         H       Me                                                    cyclo-Pr         Me      Me                                                    cyclo-Pr         H       OMe                                                   cyclo-Pr         Me      OMe                                                   cyclo-Pr         H       OCF.sub.2 H                                           cyclo-Pr         Me      OCF.sub.2 H                                           OMe              H       Me                                                    OMe              Me      Me                                                    OMe              H       OMe                                                   OMe              Me      OMe                                                   OMe              H       OCF.sub.2 H                                           OMe              Me      OCF.sub.2 H                                           OEt              H       Me                                                    OEt              Me      Me                                                    OEt              H       OMe                                                   OEt              Me      OMe                                                   OEt              H       OCF.sub.2 H                                           OEt              Me      OCF.sub.2 H                                           O-- -n-Pr        H       Me                                                    O-- -n-Pr        Me      Me                                                    O-- -n-Pr        H       OMe                                                   O-- -n-Pr        Me      OMe                                                   O-- -n-Pr        H       OCF.sub.2 H                                           O-- -n-Pr        Me      OCF.sub.2 H                                           O-- .sub.-i-Pr   H       Me                                                    O-- .sub.-i-Pr   Me      Me                                                    O-- .sub.-i-Pr   H       OMe                                                   O-- .sub.-i-Pr   Me      OMe                                                   O-- .sub.-i-Pr   H       OCF.sub.2 H                                           O-- .sub.-i-Pr   Me      OCF.sub.2 H                                           SMe              H       Me                                                    SMe              Me      Me                                                    SMe              H       OMe                                                   SMe              Me      OMe                                                   SMe              H       OCF.sub.2 H                                           SMe              Me      OCF.sub.2 H                                           SEt              H       Me                                                    SEt              Me      Me                                                    SEt              H       OMe                                                   SEt              Me      OMe                                                   SEt              H       OCF.sub.2 H                                           SEt              Me      OCF.sub.2 H                                           S-- -n-Pr        H       Me                                                    S-- -n-Pr        Me      Me                                                    S-- -n-Pr        H       OMe                                                   S-- -n-Pr        Me      OMe                                                   S-- -n-Pr        H       OCF.sub.2 H                                           S-- -n-Pr        Me      OCF.sub.2 H                                           S-- .sub.-i-Pr   H       Me                                                    S-- .sub.-i-Pr   Me      Me                                                    S-- .sub.-i-Pr   H       OMe                                                   S-- .sub.-i-Pr   Me      OMe                                                   S-- .sub.-i-Pr   H       OCF.sub.2 H                                           S-- .sub.-i-Pr   Me      OCF.sub.2 H                                           O--allyl         H       Me                                                    O--allyl         Me      Me                                                    O--allyl         H       OMe                                                   O--allyl         Me      OMe                                                   O--allyl         H       OCF.sub.2 H                                           O--allyl         Me      OCF.sub.2 H                                           O--propargyl     H       Me                                                    O--propargyl     Me      Me                                                    O--propargyl     H       OMe                                                   O--propargyl     Me      OMe                                                   O--propargyl     H       OCF.sub.2 H                                           O--propargyl     Me      OCF.sub.2 H                                           CH.sub.2 F       H       Me                                                    CH.sub.2 F       Me      Me                                                    CH.sub.2 F       H       OMe                                                   CH.sub.2 F       Me      OMe                                                   CH.sub.2 F       H       OCF.sub.2 H                                           CH.sub.2 F       Me      OCF.sub.2 H                                           CHF.sub.2        H       Me                                                    CHF.sub.2        Me      Me                                                    CHF.sub.2        H       OMe                                                   CHF.sub.2        Me      OMe                                                   CHF.sub.2        H       OCF.sub.2 H                                           CHF.sub.2        Me      OCF.sub.2 H                                           CF.sub.3         H       Me                                                    CF.sub.3         Me      Me                                                    CF.sub.3         H       OMe                                                   CF.sub.3         Me      OMe                                                   DF.sub.3         H       OCF.sub.2 H                                           CF.sub.3         Me      OCF.sub.2 H                                           CH.sub.2 Cl      H       Me                                                    CH.sub.2 Cl      Me      Me                                                    CH.sub.2 Cl      H       OMe                                                   CH.sub.2 Cl      Me      OMe                                                   CH.sub.2 Cl      H       OCF.sub.2 H                                           CH.sub.2 Cl      Me      OCF.sub.2 H                                           CHCl.sub.2       H       Me                                                    CHCl.sub.2       Me      Me                                                    CHCl.sub.2       H       OMe                                                   CHCl.sub.2       Me      OMe                                                   CHCl.sub.2       H       OCF.sub.2 H                                           CHCl.sub.2       Me      OCF.sub.2 H                                           CCl.sub.3        H       Me                                                    CCl.sub.3        Me      Me                                                    CCl.sub.3        H       OMe                                                   CCl.sub.3        Me      OMe                                                   CCl.sub.3        H       OCF.sub.2 H                                           CCl.sub.3        Me      OCF.sub.2 H                                           CHFCH.sub.3      H       Me                                                    CHFCH.sub.3      Me      Me                                                    CHFCH.sub.3      H       OMe                                                   CHFCH.sub.3      Me      OMe                                                   CHFCH.sub.3      H       OCF.sub.2 H                                           CHFCH.sub.3      Me      OCF.sub.2 H                                           CF.sub.2 CH.sub.3                                                                               H       Me                                                    CF.sub.2 CH.sub.3                                                                               Me      Me                                                    CF.sub.2 CH.sub.3                                                                               H       OMe                                                   CF.sub.2 CH.sub.3                                                                               Me      OMe                                                   CF.sub.2 CH.sub.3                                                                               H       OCF.sub.2 H                                           CF.sub.2 CH.sub.3                                                                               Me      OCF.sub.2 H                                           CH.sub.2 CH.sub.2 F                                                                             H       Me                                                    CH.sub.2 CH.sub.2 F                                                                             Me      Me                                                    CH.sub.2 CH.sub.2 F                                                                             H       OMe                                                   CH.sub.2 CH.sub.2 F                                                                             Me      OMe                                                   CH.sub.2 CH.sub.2 F                                                                             H       OCF.sub.2 H                                           CH.sub.2 CH.sub.2 F                                                                             Me      OCF.sub.2 H                                           CH.sub.2 CHF.sub.2                                                                              H       Me                                                    CH.sub.2 CHF.sub.2                                                                              Me      Me                                                    CH.sub.2 CHF.sub.2                                                                              H       OMe                                                   CH.sub.2 CHF.sub.2                                                                              Me      OMe                                                   CH.sub.2 CHF.sub.2                                                                              H       OCF.sub.2 H                                           CH.sub.2 CHF.sub.2                                                                              Me      OCF.sub.2 H                                           CH.sub.2 CF.sub.3                                                                               H       Me                                                    CH.sub.2 CF.sub.3                                                                               Me      Me                                                    CH.sub.2 CF.sub.3                                                                               H       OMe                                                   CH.sub.2 CF.sub.3                                                                               Me      OMe                                                   CH.sub.2 CF.sub.3                                                                               H       OCF.sub. 2 H                                          CH.sub.2 CF.sub.3                                                                               Me      OCF.sub.2 H                                           CHClCH.sub.3     H       Me                                                    CHClCH.sub.3     Me      Me                                                    CHClCH.sub.3     H       OMe                                                   CHClCH.sub.3     Me      OMe                                                   CHClCH.sub.3     H       OCF.sub.2 H                                           CHClCH.sub.3     Me      OCF.sub.2 H                                           CH.sub.2 OCH.sub.3                                                                              H       Me                                                    CH.sub.2 OCH.sub.3                                                                              Me      Me                                                    CH.sub.2 OCH.sub.3                                                                              H       OMe                                                   CH.sub.2 OCH.sub.3                                                                              Me      OMe                                                   CH.sub.2 OCH.sub.3                                                                              H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.3                                                                              Me      OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.3                                                                      H       Me                                                    (CH.sub.2).sub.2 OCH.sub.3                                                                      Me      Me                                                    (CH.sub.2).sub.2 OCH.sub.3                                                                      H       OMe                                                   (CH.sub.2).sub.2 OCH.sub.3                                                                      Me      OMe                                                   (CH.sub.2).sub.2 OCH.sub.3                                                                      H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.3                                                                      Me      OCF.sub.2 H                                           CH(OCH.sub.3)CH.sub.3                                                                           H       Me                                                    CH(OCH.sub.3)CH.sub.3                                                                           Me      Me                                                    CH(OCH.sub.3)CH.sub.3                                                                           H       OMe                                                   CH(OCH.sub.3)CH.sub.3                                                                           Me      OMe                                                   CH(OCH.sub.3)CH.sub.3                                                                           H       OCF.sub.2 H                                           CH(OCH.sub.3)CH.sub.3                                                                           Me      OCF.sub.2 H                                           CH.sub.2 SCH.sub.3                                                                              H       Me                                                    CH.sub.2 SCH.sub.3                                                                              Me      Me                                                    CH.sub.2 SCH.sub.3                                                                              H       OMe                                                   CH.sub.2 SCH.sub.3                                                                              Me      OMe                                                   CH.sub.2 SCH.sub.3                                                                              H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.3                                                                              Me      OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.3                                                                      H       Me                                                    (CH.sub.2).sub.2 SCH.sub.3                                                                      Me      Me                                                    (CH.sub.2).sub.2 SCH.sub.3                                                                      H       OMe                                                   (CH.sub.2).sub.2 SCH.sub.3                                                                      Me      OMe                                                   (CH.sub.2).sub.2 SCH.sub.3                                                                      Me      OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.3                                                                      Me      OCF.sub.2 H                                           CH(SCH.sub.3)CH.sub.3                                                                           H       Me                                                    CH(SCH.sub.3)CH.sub.3                                                                           Me      Me                                                    CH(SCH.sub.3)CH.sub.3                                                                           H       OMe                                                   CH(SCH.sub.3)CH.sub.3                                                                           Me      OMe                                                   CH(SCH.sub.3)CH.sub.3                                                                           H       OCF.sub.2 H                                           CH(SCH.sub.3)CH.sub.3                                                                           Me      OCF.sub.2 H                                           OCF.sub.2 H      H       Me                                                    OCF.sub.2 H      Me      Me                                                    OCF.sub.2 H      H       OMe                                                   OCF.sub.2 H      Me      OMe                                                   OCF.sub.2 H      H       OCF.sub.2 H                                           OCF.sub.2 H      Me      OCF.sub.2 H                                           OCH.sub.2 CH.sub.2 F                                                                            H       Me                                                    OCH.sub.2 CH.sub.2 F                                                                            Me      Me                                                    OCH.sub.2 CH.sub.2 F                                                                            H       OMe                                                   OCH.sub.2 CH.sub.2 F                                                                            Me      OMe                                                   OCH.sub.2 CH.sub.2 F                                                                            H       OCF.sub.2 H                                           OCH.sub.2 CH.sub.2 F                                                                            Me      OCF.sub.2 H                                           OCH.sub.2 CHF.sub.2                                                                             H       Me                                                    OCH.sub.2 CHF.sub.2                                                                             Me      Me                                                    OCH.sub.2 CHF.sub.2                                                                             H       OMe                                                   OCH.sub.2 CHF.sub.2                                                                             Me      OMe                                                   OCH.sub.2 CHF.sub.2                                                                             H       OCF.sub.2 H                                           OCH.sub.2 CHF.sub.2                                                                             Me      OCF.sub.2 H                                           OCH.sub.2 CF.sub.3                                                                              H       Me                                                    OCH.sub.2 CF.sub.3                                                                              Me      Me                                                    OCH.sub.2 CF.sub.3                                                                              H       OMe                                                   OCH.sub.2 CF.sub.3                                                                              Me      OMe                                                   OCH.sub.2 CF.sub.3                                                                              H       OCF.sub.2 H                                           OCH.sub.2 CF.sub.3                                                                              Me      OCF.sub.2 H                                           O(CH.sub.2).sub.2 Cl                                                                            H       Me                                                    O(CH.sub.2).sub.2 Cl                                                                            Me      Me                                                    O(CH.sub.2).sub.2 Cl                                                                            H       OMe                                                   O(CH.sub.2).sub.2 Cl                                                                            Me      OMe                                                   O(CH.sub.2).sub.2 Cl                                                                            H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 Cl                                                                            Me      OCF.sub.2 H                                           S(O)Me           H       Me                                                    S(O)Me           Me      Me                                                    S(O)Me           H       OMe                                                   S(O)Me           Me      OMe                                                   S(O)Me           H       OCF.sub. 2 H                                          S(O)Me           Me      OCF.sub.2 H                                           S(O)Et           H       Me                                                    S(O)Et           Me      Me                                                    S(O)Et           H       OMe                                                   S(O)Et           Me      OMe                                                   S(O)Et           H       OCF.sub.2 H                                           S(O)Et           Me      OCF.sub.2 H                                           S(O)-- -n-Pr     H       Me                                                    S(O)-- -n-Pr     Me      Me                                                    S(O)-- -n-Pr     H       OMe                                                   S(O)-- -n-Pr     Me      OMe                                                   S(O)-- -n-Pr     H       OCF.sub.2 H                                           S(O)-- -n-Pr     Me      OCF.sub.2 H                                           S(O)-- .sub.-i-Pr                                                                               H       Me                                                    S(O)-- .sub.-i-Pr                                                                               Me      Me                                                    S(O)-- .sub.-i-Pr                                                                               H       OMe                                                   S(O)-- .sub.-i-Pr                                                                               Me      Me                                                    S(O)-- .sub.-i-Pr                                                                               H       OCF.sub.2 H                                           S(O)-- .sub.-i-Pr                                                                               Me      OCF.sub.2 H                                           SO.sub.2 Me      H       Me                                                    SO.sub.2 Me      Me      Me                                                    SO.sub.2 Me      H       OMe                                                   SO.sub.2 Me      Me      OMe                                                   SO.sub.2 Me      H       OCF.sub.2 H                                           SO.sub.2 Me      Me      OCF.sub.2 H                                           SO.sub.2 Et      H       Me                                                    SO.sub.2 Et      Me      Me                                                    SO.sub.2 Et      H       OMe                                                   SO.sub.2 Et      Me      OMe                                                   SO.sub.2 Et      H       OCF.sub.2 H                                           SO.sub.2 Et      Me      OCF.sub.2 H                                           SO.sub.2 -- -n-Pr                                                                               H       Me                                                    SO.sub.2 -- -n-Pr                                                                               Me      Me                                                    SO.sub.2 -- -n-Pr                                                                               H       OMe                                                   SO.sub.2 -- -n-Pr                                                                               Me      OMe                                                   SO.sub.2 -- -n-Pr                                                                               H       OCF.sub.2 H                                           SO.sub.2 -- -n-Pr                                                                               Me      OCF.sub.2 H                                           SO.sub.2 -- .sub.-i-Pr                                                                          H       Me                                                    SO.sub.2 -- .sub.-i-Pr                                                                          Me      Me                                                    SO.sub.2 -- .sub.-i-Pr                                                                          H       OMe                                                   SO.sub.2 -- .sub.-i-Pr                                                                          Me      OMe                                                   SO.sub.2 -- .sub.-i-Pr                                                                          H       OCF.sub.2 H                                           SO.sub.2 -- .sub.-i-Pr                                                                          Me      OCF.sub.2 H                                           S--allyl         H       Me                                                    S--allyl         Me      Me                                                    S--allyl         H       OMe                                                   S--allyl         Me      OMe                                                   S--allyl         H       OCF.sub.2 H                                           S--allyl         Me      OCF.sub.2 H                                           S(O)allyl        H       Me                                                    S(O)allyl        Me      Me                                                    S(O)allyl        H       OMe                                                   S(O)allyl        Me      OMe                                                   S(O)allyl        H       OCF.sub.2 H                                           S(O)allyl        Me      OCF.sub.2 H                                           SO.sub.2 allyl   H       Me                                                    SO.sub.2 allyl   Me      Me                                                    SO.sub.2 allyl   H       OMe                                                   SO.sub.2 allyl   Me      OMe                                                   SO.sub.2 allyl   H       OCF.sub.2 H                                           SO.sub.2 allyl   Me      OCF.sub.2 H                                           S--propargyl     H       Me                                                    S--propargyl     Me      Me                                                    S--propargyl     H       OMe                                                   S--propargyl     Me      OMe                                                   S--propargyl     H       OCF.sub.2 H                                           S--propargyl     Me      OCF.sub.2 H                                           S(O)propargyl    H       Me                                                    S(O)propargyl    Me      Me                                                    S(O)propargyl    H       OMe                                                   S(O)propargyl    Me      OMe                                                   S(O)propargyl    H       OCF.sub.2 H                                           S(O)propargyl    Me      OCF.sub.2 H                                           SO.sub.2 propargyl                                                                              H       Me                                                    SO.sub.2 propargyl                                                                              Me      Me                                                    SO.sub.2 propargyl                                                                              H       OMe                                                   SO.sub.2 propargyl                                                                              Me      OMe                                                   SO.sub.2 propargyl                                                                              H       OCF.sub.2 H                                           SO.sub.2 propargyl                                                                              Me      OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       Me                                                    CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       OMe                                                   CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       Me                                                    (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       OMe                                                   (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             CH.sub.3                                                                               Me                                                    CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                  H       Me                                                    CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CF.sub.3                                                                     H       Me                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                     H       OMe                                                   CH.sub.2 OCH.sub.2 CF.sub.3                                                                     H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                           H       Me                                                    (CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                           H       OMe                                                   CH.sub.2 OCF.sub.2 H                                                                            H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                   CH.sub.3                                                                               OMe                                                   CH.sub.2 OCH.sub.2 CHF.sub.2                                                                    H       Me                                                    CH.sub.2 OCH.sub.2 CH.sub.2 Br                                                                  H       OMe                                                   CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                  H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.2 I                                                                   H       Me                                                    CH.sub.2 OCF.sub.3                                                                              H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       Me                                                    CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       OMe                                                   (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             H       OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             CH.sub.3                                                                               OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             H       Me                                                    (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             H       OMe                                                   CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       Me                                                    CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       Me                                                    CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       OMe                                                   (CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                           H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                   H       OMe                                                   CH(CH.sub.3)S(O).sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           CH.sub.3                                                                               Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                 H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                   H       OMe                                                   CH.sub.2 S(O).sub.2 CF.sub.2 H                                                                  H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 F                                                         H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CHF.sub.2                                                          H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 Br                                                        H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 I                                                         CH.sub.3                                                                               OMe                                                   CH.sub.2 S(O).sub.2 CF.sub.3                                                                    H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                 H       OMe                                                   OCH.sub.2 OCH.sub.3                                                                             H       OCF.sub.2 H                                           OCH.sub.2 OCH.sub.3                                                                             H       Me                                                    OCH.sub.2 OCH.sub.3                                                                             H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       Me                                                    O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            CH.sub.3                                                                               OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       Me                                                    O(CH.sub.2 ).sub.2 OCH.sub.2 CH.sub.3                                                           H       OMe                                                   OCH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                             H       Me                                                    CH.sub.2 SCF.sub.2 H                                                                            H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.2 F                                                                   H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CHF.sub.2                                                                    H       Me                                                    CH.sub.2 SCH.sub.2 CH.sub.2 Br                                                                  H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.2 Cl                                                                  H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CH.sub.2 I                                                                   CH.sub.3                                                                               Me                                                    CH.sub.2 SCF.sub.3                                                                              H       Me                                                    CH.sub.2 S(O)CH.sub.3                                                                           H       OMe                                                   CH.sub.2 S(O)CH.sub.3                                                                           H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.3                                                                           H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       OMe                                                   (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       Me                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  CH.sub.3                                                                               OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                          H       OMe                                                   CH(CH.sub.3 S(O)CH.sub.3                                                                        H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                  H       Me                                                    CH.sub.2 S(O)CH.sub. 2 CF.sub.3                                                                 H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                  H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                        H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                          H       OMe                                                   CH.sub.2 S(O)CF.sub.2 H                                                                         H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CH.sub.2 F                                                                CH.sub.3                                                                               OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CHF.sub.2                                                                 H       Me                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.2 Br                                                               H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.2 I                                                                H       OCF.sub.2 H                                           CH.sub.2 S(O)CF.sub.3                                                                           H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       OMe                                                   (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           OCH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       Me                                                    O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                          H       Me                                                    O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                          H       OMe                                                   O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                           H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCF.sub.3                                                                     H       Me                                                    OCH.sub.2 SCH.sub.3                                                                             H       OMe                                                   OCH.sub.2 SCH.sub.3                                                                             H       OCF.sub.2 H                                           OCH.sub.2 SCH.sub.3                                                                             H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OMe                                                   O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 SCH.sub.3                                                                     CH.sub.3                                                                               Me                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                   O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       Me                                                    OCH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OMe                                                   OCH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OMe                                                   O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                          H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                          CH.sub.3                                                                               OMe                                                   O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                           H       Me                                                    O(CH.sub.2).sub.2 SCF.sub.3                                                                     H       OMe                                                   OCH.sub.2 S(O)CH.sub.3                                                                          H       OCF.sub.2 H                                           OCH.sub.2 S(O)CH.sub.3                                                                          H       Me                                                    OCH.sub.2 S(O)CH.sub. 3                                                                         H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       Me                                                    O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         CH.sub.3                                                                               OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         H       Me                                                    OCH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                         H       OCF.sub.2 H                                           OCH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       Me                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                       H       OMe                                                   O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Cl                                                       H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Br                                                       H       Me                                                    O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 I                                                        H       OMe                                                   O(CH.sub.2).sub.2 S(O)CF.sub.3                                                                  H       OCF.sub.2 H                                           OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OMe                                                   OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  CH.sub.3                                                                               Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OCF.sub.2 H                                           OCH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                  H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Cl                                                H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Br                                                H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 I                                                 CH.sub.3                                                                               OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CF.sub.3                                                           H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                H       OMe                                                   OCH.sub.2 S(O).sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 CN                                                                            H       Me                                                    O(CH.sub.2).sub.2 CN                                                                            H       OMe                                                   O(CH.sub.2).sub.2 CN                                                                            H       OCF.sub.2 H                                           OCH.sub.2 CN     H       Me                                                    OCH.sub.2 CN     H       OMe                                                   OCH.sub.2 CN     H       OCF.sub.2 H                                           OCH.sub.2 CN     CH.sub.3                                                                               OCF.sub.2 H                                           OCH(CH.sub.3)CN  H       Me                                                    O(CH.sub.2).sub.2 NH.sub.2                                                                      H       OMe                                                   O(CH.sub.2).sub.2 NH.sub.2                                                                      H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 NH.sub.2                                                                      H       Me                                                    O(CH.sub.2).sub.2 NHCH.sub.3                                                                    H       OMe                                                   O(CH.sub.2).sub.2 NHCH.sub.3                                                                    H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 NHCH.sub.3                                                                    H       Me                                                    O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       OMe                                                   O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       Me                                                    SCH.sub.2 OCH.sub.3                                                                             H       OMe                                                   SCH.sub.2 OCH.sub.3                                                                             H       OCF.sub.2 H                                           SCH.sub.2 OCH.sub.3                                                                             H       Me                                                    SCH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OMe                                                   S(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 OCH.sub.3                                                                     CH.sub.3                                                                               Me                                                    S(CH.sub.2).sub.2 OCH.sub.3                                                                     H       Me                                                    S(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OMe                                                   S(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       Me                                                    SCH.sub.2 OCH.sub. 2 CF.sub.3                                                                   H       OMe                                                   S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                          H       Me                                                    S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                          H       OMe                                                   S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                           H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 OCF.sub.3                                                                     CH.sub.3                                                                               OMe                                                   SCH.sub.2 SCH.sub.3                                                                             H       Me                                                    SCH.sub.2 SCH.sub.3                                                                             H       OMe                                                   SCH.sub.2 SCH.sub.3                                                                             H       OCF.sub.2 H                                           SCH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OMe                                                   S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                   SCH(CH.sub.3)SCH.sub.3                                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            CH.sub.3                                                                               OCF.sub.2 H                                           SCH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OMe                                                   S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                          H       Me                                                    S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                           H       OMe                                                   S(CH.sub.2).sub.2 SCF.sub.3                                                                     H       OCF.sub.2 H                                           SCH.sub.2 CN     H       Me                                                    SCH.sub.2 CN     H       OMe                                                   SCH.sub.2 CN     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CN                                                                            H       Me                                                    S(CH.sub.2).sub.2 CN                                                                            H       OMe                                                   S(CH.sub.2).sub.2 CN                                                                            H       OCF.sub.2 H                                           SCH(CH.sub.3)CN  H       Me                                                    SCHF.sub.2       H       OMe                                                   SCHF.sub.2       H       OCF.sub.2 H                                           SCHF.sub.2       CH.sub.3                                                                               Me                                                    SCHF.sub.2       H       Me                                                    SCF.sub.3        H       OMe                                                   SCH.sub.2 CFH    H       OCF.sub.2 H                                           SCH.sub.2 CF.sub.2 H                                                                            H       Me                                                    SCH.sub.2 CF.sub.3                                                                              H       OMe                                                   SCH.sub.2 CF.sub.3                                                                              H       OCF.sub.2 H                                           SCH.sub.2 CF.sub.3                                                                              H       Me                                                    SCH.sub.2 CF.sub.2 H                                                                            H       OMe                                                   S(CH.sub.2).sub.2 CFH.sub.2                                                                     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CClH.sub.2                                                                    CH.sub.3                                                                               OMe                                                   S(CH.sub.2).sub.2 CIH.sub.2                                                                     H       Me                                                    SCF.sub.2 CF.sub.3                                                                              H       OMe                                                   SCH(CH.sub.3)CF.sub.3                                                                           H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CCl.sub.3                                                                     H       Me                                                    S(O)CHF.sub.2    H       OMe                                                   S(O)CHF.sub.2    H       OCF.sub.2 H                                           S(O)CHF.sub.2    H       Me                                                    S(O)CF.sub.3     H       OMe                                                   S(O)CH.sub.2 CFH.sub.2                                                                          H       OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.2 H                                                                         CH.sub.3                                                                               OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.3                                                                           H       Me                                                    S(O)CH.sub.2 CF.sub.3                                                                           H       OMe                                                   S(O)CH.sub.2 CF.sub.3                                                                           H       OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.2 H                                                                         H       Me                                                    S(O)(CH.sub.2).sub.2 CFH.sub.2                                                                  H       OMe                                                   S(O)(CH.sub.2).sub.2 CClH.sub.2                                                                 H       OCF.sub.2 H                                           S(O)(CH.sub.2).sub.2 CIH.sub.2                                                                  H       Me                                                    S(O)CF.sub.2 CF.sub.3                                                                           H       OMe                                                   S(O)CH(CH.sub.3)CF.sub.3                                                                        H       OCF.sub.2 H                                           S(O)(CH.sub.2).sub.2 CCl.sub.3                                                                  H       Me                                                    S(O).sub.2 CHF.sub.2                                                                            H       OMe                                                   S(O).sub.2 CHF.sub.2                                                                            H       OCF.sub.2 H                                           S(O).sub.2 CHF.sub.2                                                                            H       Me                                                    S(O).sub.2 CF.sub.3                                                                             H       OMe                                                   S(O).sub.2 CH.sub.2 CFH.sub.2                                                                   H       OCF.sub.2 H                                           S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                  CH.sub.3                                                                               Me                                                    S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       Me                                                    S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       OMe                                                   S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                  H       Me                                                    S(O).sub.2 (CH.sub.2).sub.2 CFH.sub.2                                                           H       OMe                                                   S(O).sub.2 (CH.sub.2).sub.2 CClH.sub.2                                                          H       OCF.sub.2 H                                           S(O).sub.2 (CH.sub.2).sub.2 CIH.sub.2                                                           H       Me                                                    S(O).sub.2 CF.sub.2 CF.sub.3                                                                    H       OMe                                                   S(O).sub.2 CH(CH.sub.3)CF.sub.3                                                                 H       OCF.sub.2 H                                           S(O).sub.2 (CH.sub.2).sub.2 CCl.sub.3                                                           CH.sub.3                                                                               OMe                                                   S(O).sub.2 CH.sub.2 Cl                                                                          H       Me                                                    CH═CH.sub.2  H       OMe                                                   CH═CH.sub.2  H       OCF.sub.2 H                                           CH═CH.sub.2  H       Me                                                    CH.sub.2 CH═CH.sub.2                                                                        H       OMe                                                   CH.sub.2 CH═CH.sub.2                                                                        H       OCF.sub.2 H                                           CH.sub.2 CH═CH.sub.2                                                                        H       Me                                                    CH═CHCH.sub.3                                                                               H       OMe                                                   C(CH.sub.3)═CH.sub.2                                                                        H       OCF.sub.2 H                                           CH═CH.sub.2  CH.sub.3                                                                               OCF.sub.2 H                                           CH.tbd.CH        H       Me                                                    CH.tbd.CH        H       OMe                                                   CH.tbd.CH        H       OCF.sub.2 H                                           CH.sub.2 C.tbd.CH                                                                               H       Me                                                    CH.sub.2 C.tbd.CH                                                                               H       OMe                                                   CH.sub.2 C.tbd.CH                                                                               H       OCF.sub.2 H                                           C.tbd.CCH.sub.3  H       Me                                                    C.tbd.CCH.sub.3  H       OMe                                                   C.tbd.CCH.sub.3  H       OCF.sub.2 H                                           NH.sub.2         H       Me                                                    NH.sub.2         H       OMe                                                   NH.sub.2         H       OCF.sub.2 H                                           NHCH.sub.3       H       Me                                                    NHCH.sub.3       H       OMe                                                   NHCH.sub.3       H       OCF.sub.2 H                                           NHCH.sub.3       CH.sub.3                                                                               Me                                                    N(CH.sub.3).sub.2                                                                               H       Me                                                    N(CH.sub.3).sub.2                                                                               H       OMe                                                   N(CH.sub.3).sub.2                                                                               H       OCF.sub.2 H                                           NHCH.sub.2 CH.sub.3                                                                             H       Me                                                    NHCH.sub.2 CH.sub.3                                                                             H       OMe                                                   NHCH.sub.2 CH.sub.3                                                                             H       OCF.sub.2 H                                           N(CH.sub.3)CH.sub.2 CH.sub.3                                                                    H       Me                                                    N(CH.sub.2 CH.sub.3).sub.2                                                                      H       OMe                                                   NHCH.sub.2 CF.sub.3                                                                             H       OCF.sub.2 H                                           NHCH.sub.2 CF.sub.3                                                                             CH.sub.3                                                                               OMe                                                   NHCH.sub.2 CF.sub.3                                                                             H       Me                                                    NHCH.sub.2 CF.sub.3                                                                             H       OMe                                                   N(CH.sub.3)CH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           N(CH.sub.3)CH.sub.2 CHF.sub.2                                                                   H       Me                                                    N(CH.sub.3)(CH.sub.2).sub.2 F                                                                   H       OMe                                                   N(CH.sub.3)(CH.sub.2).sub.2 Cl                                                                  H       OCF.sub.2 H                                           N(CH.sub.3)(CH.sub.2).sub.2 I                                                                   H       Me                                                    N(CH.sub.3)(CH.sub.2).sub.2 Br                                                                  H       OMe                                                   NHCF.sub.3       CH.sub.3                                                                               OCF.sub.2 H                                           NHCF.sub.3       H       Me                                                    NH(CH.sub.2).sub.2 F                                                                            H       OMe                                                   N(CH.sub.3)CF.sub.2 H                                                                           H       OCF.sub.2 H                                           NHCF.sub.2 H     H       Me                                                    ______________________________________                                    

                  TABLE VIIa                                                       ______________________________________                                         R.sub.1 = CH.sub.2 CH.sub.2 Cl                                                 R.sub.2          R       Y         m.p. (°C.)                           ______________________________________                                         Me               H       Me                                                    Me               Me      Me                                                    Me               H       OMe                                                   Me               Me      OMe                                                   Me               H       OCF.sub.2 H                                           Me               Me      OCF.sub.2 H                                           Et               H       Me                                                    Et               Me      Me                                                    Et               H       OMe                                                   Et               Me      OMe                                                   Et               H       OCF.sub.2 H                                           Et               Me      OCF.sub.2 H                                           Pr               H       Me                                                    Pr               Me      Me                                                    Pr               H       OMe                                                   Pr               Me      OMe                                                   Pr               H       OCF.sub.2 H                                           Pr               Me      OCF.sub.2 H                                            .sub.-i-Pr      H       Me                                                     .sub.-i-Pr      Me      Me                                                     .sub.-i-Pr      H       OMe                                                    .sub.-i-Pr      Me      OMe                                                    .sub.-i-Pr      H       OCF.sub.2 H                                            .sub.-i-Pr      Me      OCF.sub.2 H                                           cyclo-Pr         H       Me                                                    cyclo-Pr         Me      Me                                                    cyclo-Pr         H       OMe                                                   cyclo-Pr         Me      OMe                                                   cyclo-Pr         H       OCF.sub.2 H                                           cyclo-Pr         Me      OCF.sub.2 H                                           OMe              H       Me                                                    OMe              Me      Me                                                    OMe              H       OMe                                                   OMe              Me      OMe                                                   OMe              H       OCF.sub.2 H                                           OMe              Me      OCF.sub.2 H                                           OEt              H       Me                                                    OEt              Me      Me                                                    OEt              Me      OMe                                                   OEt              Me      OMe                                                   OEt              H       OCF.sub.2 H                                           OEt              Me      OCF.sub.2 H                                           O-- -n-Pr        H       Me                                                    O-- -n-Pr        Me      Me                                                    O-- -n-Pr        H       OMe                                                   O-- -n-Pr        Me      OMe                                                   O-- -n-Pr        H       OCF.sub.2 H                                           O-- -n-Pr        Me      OCF.sub.2 H                                           O-- .sub.-i-Pr   H       Me                                                    O-- .sub.-i-Pr   Me      Me                                                    O-- .sub.-i-Pr   H       OMe                                                   O-- .sub.-i-Pr   Me      OMe                                                   O-- .sub.-i-Pr   H       OCF.sub.2 H                                           O-- .sub.-i-Pr   Me      OCF.sub.2 H                                           SMe              H       Me                                                    SMe              Me      Me                                                    SMe              H       OMe                                                   SMe              Me      OMe                                                   SMe              H       OCF.sub.2 H                                           SMe              Me      OCF.sub.2 H                                           SEt              H       Me                                                    SEt              Me      Me                                                    SEt              H       OMe                                                   SEt              Me      OMe                                                   SEt              H       OCF.sub.2 H                                           SEt              Me      OCF.sub.2 H                                           S-- -n-Pr        H       Me                                                    S-- -n-Pr        Me      Me                                                    S-- -n-Pr        H       OMe                                                   S-- -n-Pr        Me      OMe                                                   S-- -n-Pr        H       OCF.sub.2 H                                           S-- -n-Pr        Me      OCF.sub.2 H                                           S-- .sub.-i-Pr   H       Me                                                    S-- .sub.-i-Pr   Me      Me                                                    S-- .sub.-i-Pr   H       OMe                                                   S-- .sub.-i-Pr   Me      OMe                                                   S-- .sub.-i-Pr   H       OCF.sub.2 H                                           S-- .sub.-i-Pr   Me      OCF.sub.2 H                                           O--allyl         H       Me                                                    O--allyl         Me      Me                                                    O--allyl         H       OMe                                                   O--allyl         Me      OMe                                                   O--allyl         H       OCF.sub.2 H                                           O--allyl         Me      OCF.sub.2 H                                           O--propargyl     H       Me                                                    O--propargyl     Me      Me                                                    O--propargyl     H       OMe                                                   O--propargyl     Me      OMe                                                   O--propargyl     H       OCF.sub.2 H                                           O--propargyl     Me      OCF.sub.2 H                                           CH.sub.2 F       H       Me                                                    CH.sub.2 F       Me      Me                                                    CH.sub.2 F       H       OMe                                                   CH.sub.2 F       Me      OMe                                                   CH.sub.2 F       H       OCF.sub.2 H                                           CH.sub.2 F       Me      OCF.sub.2 H                                           CHF.sub.2        H       Me                                                    CHF.sub.2        Me      Me                                                    CHF.sub.2        H       OMe                                                   CHF.sub.2        Me      OMe                                                   CHF.sub.2        H       OCF.sub.2 H                                           CHF.sub.2        Me      OCF.sub.2 H                                           CF.sub.3         H       Me                                                    CF.sub.3         Me      Me                                                    CF.sub.3         H       OMe                                                   CF.sub.3         Me      OMe                                                   CF.sub.3         H       OCF.sub.2 H                                           CF.sub.3         Me      OCF.sub.2 H                                           CH.sub.2 Cl      H       Me                                                    CH.sub.2 Cl      Me      Me                                                    CH.sub.2 Cl      H       OMe                                                   CH.sub.2 Cl      Me      OMe                                                   CH.sub.2 Cl      H       OCF.sub.2 H                                           CH.sub.2 Cl      Me      OCF.sub.2 H                                           CHCl.sub.2       H       Me                                                    CHCl.sub.2       Me      Me                                                    CHCl.sub.2       H       OMe                                                   CHCl.sub.2       Me      OMe                                                   CHCl.sub.2       H       OCF.sub.2 H                                           CHCl.sub.2       Me      OCF.sub.2 H                                           CCl.sub.3        H       Me                                                    CCl.sub.3        Me      Me                                                    CCl.sub.3        H       OMe                                                   CCl.sub.3        Me      OMe                                                   CCl.sub.3        H       OCF.sub.2 H                                           CCl.sub.3        Me      OCF.sub.2 H                                           CHFCH.sub.3      H       Me                                                    CHFCH.sub.3      Me      Me                                                    CHFCH.sub.3      H       OMe                                                   CHFCH.sub.3      Me      OMe                                                   CHFCH.sub.3      H       OCF.sub.2 H                                           CHFCH.sub.3      Me      OCF.sub.2 H                                           CF.sub.2 CH.sub.3                                                                               H       Me                                                    CF.sub.2 CH.sub.3                                                                               Me      Me                                                    CF.sub.2 CH.sub.3                                                                               H       OMe                                                   CF.sub.2 CH.sub.3                                                                               Me      OMe                                                   CF.sub.2 CH.sub.3                                                                               H       OCF.sub.2 H                                           CF.sub.2 CH.sub.3                                                                               Me      OCF.sub.2 H                                           CH.sub.2 CH.sub.2 F                                                                             H       Me                                                    CH.sub.2 CH.sub.2 F                                                                             Me      Me                                                    CH.sub.2 CH.sub.2 F                                                                             H       OMe                                                   CH.sub.2 CH.sub.2 F                                                                             Me      OMe                                                   CH.sub.2 CH.sub.2 F                                                                             H       OCF.sub.2 H                                           CH.sub.2 CH.sub.2 F                                                                             Me      OCF.sub.2 H                                           CH.sub.2 CHF.sub.2                                                                              H       Me                                                    CH.sub.2 CHF.sub.2                                                                              Me      Me                                                    CH.sub.2 CHF.sub.2                                                                              H       OMe                                                   CH.sub.2 CHF.sub.2                                                                              Me      OMe                                                   CH.sub.2 CHF.sub.2                                                                              H       OCF.sub.2 H                                           CH.sub.2 CHF.sub.2                                                                              Me      OCF.sub.2 H                                           CH.sub.2 CF.sub.3                                                                               H       Me                                                    CH.sub.2 CF.sub.3                                                                               Me      Me                                                    CH.sub.2 CF.sub.3                                                                               H       OMe                                                   CH.sub.2 CF.sub.3                                                                               Me      OMe                                                   CH.sub.2 CF.sub.3                                                                               H       OCF.sub.2 H                                           CH.sub.2 CF.sub.3                                                                               Me      OCF.sub.2 H                                           CHClCH.sub.3     H       Me                                                    CHClCH.sub.3     Me      Me                                                    CHClCH.sub.3     H       OMe                                                   CHClCH.sub.3     Me      OMe                                                   CHClCH.sub.3     H       OCF.sub.2 H                                           CHClCH.sub.3     Me      OCF.sub.2 H                                           CH.sub.2 OCH.sub.3                                                                              H       Me                                                    CH.sub.2 OCH.sub.3                                                                              Me      Me                                                    CH.sub.2 OCH.sub.3                                                                              H       OMe                                                   CH.sub.2 OCH.sub.3                                                                              Me      OMe                                                   CH.sub.2 OCH.sub.3                                                                              H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.3                                                                              Me      OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.3                                                                      H       Me                                                    (CH.sub.2).sub.2 OCH.sub.3                                                                      Me      Me                                                    (CH.sub.2).sub.2 OCH.sub.3                                                                      H       OMe                                                   (CH.sub.2).sub.2 OCH.sub.3                                                                      Me      OMe                                                   (CH.sub.2).sub.2 OCH.sub.3                                                                      H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.3                                                                      Me      OCF.sub.2 H                                           CH(OCH.sub.3)CH.sub.3                                                                           H       Me                                                    CH(OCH.sub.3)CH.sub.3                                                                           Me      Me                                                    CH(OCH.sub.3)CH.sub.3                                                                           H       OMe                                                   CH(OCH.sub.3)CH.sub.3                                                                           Me      OMe                                                   CH(OCH.sub.3)CH.sub.3                                                                           H       OCF.sub.2 H                                           CH(OCH.sub.3)CH.sub.3                                                                           Me      OCF.sub.2 H                                           CH.sub.2 SCH.sub.3                                                                              H       Me                                                    CH.sub.2 SCH.sub.3                                                                              Me      Me                                                    CH.sub.2 SCH.sub.3                                                                              H       OMe                                                   CH.sub.2 SCH.sub.3                                                                              Me      OMe                                                   CH.sub.2 SCH.sub.3                                                                              H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.3                                                                              Me      OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.3                                                                      H       Me                                                    (CH.sub.2).sub.2 SCH.sub.3                                                                      Me      Me                                                    (CH.sub.2).sub.2 SCH.sub.3                                                                      H       OMe                                                   (CH.sub.2).sub.2 SCH.sub.3                                                                      Me      OMe                                                   (CH.sub.2).sub.2 SCH.sub.3                                                                      H       OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.3                                                                      Me      OCF.sub.2 H                                           CH(SCH.sub.3)CH.sub.3                                                                           H       Me                                                    CH(SCH.sub.3)CH.sub.3                                                                           Me      Me                                                    CH(SCH.sub.3)CH.sub.3                                                                           H       OMe                                                   CH(SCH.sub.3)CH.sub.3                                                                           Me      OMe                                                   CH(SCH.sub.3)CH.sub.3                                                                           H       OCF.sub.2 H                                           CH(SCH.sub.3)CH.sub.3                                                                           Me      OCF.sub.2 H                                           OCF.sub.2 H      H       Me                                                    OCF.sub.2 H      Me      Me                                                    OCF.sub.2 H      H       OMe                                                   OCF.sub.2 H      Me      OMe                                                   OCF.sub.2 H      H       OCF.sub.2 H                                           OCF.sub.2 H      Me      OCF.sub.2 H                                           OCH.sub.2 CH.sub.2 F                                                                            H       Me                                                    OCH.sub.2 CH.sub.2 F                                                                            Me      Me                                                    OCH.sub.2 CH.sub.2 F                                                                            H       OMe                                                   OCH.sub.2 CH.sub.2 F                                                                            Me      OMe                                                   OCH.sub.2 CH.sub.2 F                                                                            H       OCF.sub.2 H                                           OCH.sub.2 CH.sub.2 F                                                                            Me      OCF.sub.2 H                                           OCH.sub.2 CHF.sub.2                                                                             H       Me                                                    OCH.sub.2 CHF.sub.2                                                                             Me      Me                                                    OCH.sub.2 CHF.sub.2                                                                             H       OMe                                                   OCH.sub.2 CHF.sub.2                                                                             Me      OMe                                                   OCH.sub.2 CHF.sub.2                                                                             H       OCF.sub.2 H                                           OCH.sub.2 CHF.sub.2                                                                             Me      OCF.sub.2 H                                           OCH.sub.2 CF.sub.3                                                                              H       Me                                                    OCH.sub.2 CF.sub.3                                                                              Me      Me                                                    OCH.sub.2 CF.sub.3                                                                              H       OMe                                                   OCH.sub.2 CF.sub.3                                                                              Me      OMe                                                   OCH.sub.2 CF.sub.3                                                                              H       OCF.sub.2 H                                           OCH.sub.2 CF.sub.3                                                                              Me      OCF.sub.2 H                                           O(CH.sub.2).sub.2 Cl                                                                            H       Me                                                    O(CH.sub.2).sub.2 Cl                                                                            Me      Me                                                    O(CH.sub.2).sub.2 Cl                                                                            H       OMe                                                   O(CH.sub.2).sub.2 Cl                                                                            Me      OMe                                                   O(CH.sub.2).sub.2 Cl                                                                            H       OCF.sub.2 H                                           O(CH.sub.2).sub. 2 Cl                                                                           Me      OCF.sub.2 H                                           S(O)Me           H       Me                                                    S(O)Me           Me      Me                                                    S(O)Me           H       OMe                                                   S(O)Me           Me      OMe                                                   S(O)Me           H       OCF.sub.2 H                                           S(O)Me           Me      OCF.sub.2 H                                           S(O)Et           H       Me                                                    S(O)Et           Me      Me                                                    S(O)Et           H       OMe                                                   S(O)Et           Me      OMe                                                   S(O)Et           H       OCF.sub.2 H                                           S(O)Et           Me      OCF.sub.2 H                                           S(O)-- -n-Pr     H       Me                                                    S(O)-- -n-Pr     Me      Me                                                    S(O)-- -n-Pr     H       OMe                                                   S(O)-- -n-Pr     Me      OMe                                                   S(O)-- -n-Pr     H       OCF.sub.2 H                                           S(O)-- -n-Pr     Me      OCF.sub.2 H                                           S(O)-- .sub.-i-Pr                                                                               H       Me                                                    S(O)-- .sub.-i-Pr                                                                               Me      Me                                                    S(O)-- .sub.-i-Pr                                                                               H       OMe                                                   S(O)-- .sub.-i-Pr                                                                               Me      Me                                                    S(O)-- .sub.-i-Pr                                                                               H       OCF.sub.2 H                                           S(O)-- .sub.-i-Pr                                                                               Me      OCF.sub.2 H                                           SO.sub.2 Me      H       Me                                                    SO.sub.2 Me      Me      Me                                                    SO.sub.2 Me      H       OMe                                                   SO.sub.2 Me      Me      OMe                                                   SO.sub.2 Me      H       OCF.sub.2 H                                           SO.sub.2 Me      Me      OCF.sub.2 H                                           SO.sub.2 Et      H       Me                                                    SO.sub. 2 Et     Me      Me                                                    SO.sub.2 Et      H       OMe                                                   SO.sub.2 Et      Me      OMe                                                   SO.sub.2 Et      H       OCF.sub.2 H                                           SO.sub.2 Et      Me      OCF.sub.2 H                                           SO.sub.2 -- -n-Pr                                                                               H       Me                                                    SO.sub.2 -- -n-Pr                                                                               Me      Me                                                    SO.sub.2 -- -n-Pr                                                                               H       OMe                                                   SO.sub.2 -- -n-Pr                                                                               Me      OMe                                                   SO.sub.2 -- -n-Pr                                                                               H       OCF.sub.2 H                                           SO.sub.2 -- -n-Pr                                                                               Me      OCF.sub.2 H                                           SO.sub.2 -- .sub.-i-Pr                                                                          H       Me                                                    SO.sub.2 -- .sub.-i-Pr                                                                          Me      Me                                                    SO.sub.2 -- .sub.-i-Pr                                                                          H       OMe                                                   SO.sub.2 -- .sub.-i-Pr                                                                          Me      OMe                                                   SO.sub.2 -- .sub.-i-Pr                                                                          H       OCF.sub.2 H                                           SO.sub.2 -- .sub.-i-Pr                                                                          Me      OCF.sub.2 H                                           S--allyl         H       Me                                                    S--allyl         Me      Me                                                    S--allyl         H       OMe                                                   S--allyl         Me      OMe                                                   S--allyl         H       OCF.sub.2 H                                           S--allyl         Me      OCF.sub.2 H                                           S(O)allyl        H       Me                                                    S(O)allyl        Me      Me                                                    S(O)allyl        H       OMe                                                   S(O)allyl        Me      OMe                                                   S(O)allyl        H       OCF.sub.2 H                                           S(O)allyl        Me      OCF.sub.2 H                                           SO.sub.2 allyl   H       Me                                                    SO.sub.2 allyl   Me      Me                                                    SO.sub.2 allyl   H       OMe                                                   SO.sub.2 allyl   Me      OMe                                                   SO.sub.2 allyl   H       OCF.sub.2 H                                           SO.sub.2 allyl   Me      OCF.sub.2 H                                           S--propargyl     H       Me                                                    S--propargyl     Me      Me                                                    S--propargyl     H       OMe                                                   S--propargyl     Me      OMe                                                   S--propargyl     H       OCF.sub.2 H                                           S--propargyl     Me      OCF.sub.2 H                                           S(O)propargyl    H       Me                                                    S(O)propargyl    Me      Me                                                    S(O)propargyl    H       OMe                                                   S(O)propargyl    Me      OMe                                                   S(O)propargyl    H       OCF.sub.2 H                                           S(O)propargyl    Me      OCF.sub.2 H                                           SO.sub.2 propargyl                                                                              H       Me                                                    SO.sub.2 propargyl                                                                              Me      Me                                                    SO.sub.2 propargyl                                                                              H       OMe                                                   SO.sub.2 propargyl                                                                              Me      OMe                                                   SO.sub.2 propargyl                                                                              H       OCF.sub.2 H                                           SO.sub.2 propargyl                                                                              Me      OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       Me                                                    CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       OMe                                                   CH.sub.2 OCH.sub.2 CH.sub.3                                                                     H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       Me                                                    (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       OMe                                                   (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                             CH.sub.3                                                                               Me                                                    CH(CH.sub. 3)OCH.sub.2 CH.sub.3                                                                 H       Me                                                    CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CF.sub.3                                                                     H       Me                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                     H       OMe                                                   CH.sub.2 OCH.sub.2 CF.sub.3                                                                     H       OCF.sub.2 H                                           (CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                           H       Me                                                    (CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                             H       OMe                                                   CH.sub.2 OCF.sub.2 H                                                                            H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                   CH.sub.3                                                                               OMe                                                   CH.sub.2 OCH.sub.2 CHF.sub.2                                                                    H       Me                                                    CH.sub.2 OCH.sub.2 CH.sub.2 Br                                                                  H       OMe                                                   CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                  H       OCF.sub.2 H                                           CH.sub.2 OCH.sub.2 CH.sub.2 I                                                                   H       Me                                                    CH.sub.2 OCF.sub.3                                                                              H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       Me                                                    CH.sub.2 SCH.sub.2 CH.sub.3                                                                     H       OMe                                                   (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             H       OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             CH.sub.3                                                                               OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                             H       Me                                                    (CH.sub.2).sub.2 SCH.sub. 2 CH.sub.3                                                            H       OMe                                                   CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       Me                                                    CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       Me                                                    CH.sub.2 SCH.sub.2 CF.sub.3                                                                     H       OMe                                                   (CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                           H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                           H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                   H       OMe                                                   CH(CH.sub.3)S(O).sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           CH.sub.3                                                                               Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                           H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                 H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                   H       OMe                                                   CH.sub.2 S(O).sub.2 CF.sub.2 H                                                                  H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 F                                                         H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CHF.sub.2                                                          H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 Br                                                        H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 I                                                         CH.sub.3                                                                               OMe                                                   CH.sub.2 S(O).sub.2 CF.sub.3                                                                    H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                 H       OMe                                                   OCH.sub.2 OCH.sub.3                                                                             H       OCF.sub.2 H                                           OCH.sub.2 OCH.sub.3                                                                             H       Me                                                    OCH.sub.2 OCH.sub.3                                                                             H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       Me                                                    O(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            CH.sub.3                                                                               OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       Me                                                    O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OMe                                                   OCH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                           (CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                             H       Me                                                    CH.sub.2 SCF.sub.2 H                                                                            H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.2 F                                                                   H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CHF.sub.2                                                                    H       Me                                                    CH.sub.2 SCH.sub.2 CH.sub.2 Br                                                                  H       OMe                                                   CH.sub.2 SCH.sub.2 CH.sub.2 Cl                                                                  H       OCF.sub.2 H                                           CH.sub.2 SCH.sub.2 CH.sub.2 I                                                                   CH.sub.3                                                                               Me                                                    CH.sub.2 SCF.sub.3                                                                              H       Me                                                    CH.sub.2 S(O)CH.sub.3                                                                           H       OMe                                                   CH.sub.2 S(O)CH.sub.3                                                                           H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.3                                                                           H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       OMe                                                   (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O)CH.sub.3                                                                   H       Me                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  CH.sub.3                                                                               OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                  H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                          H       OMe                                                   CH(CH.sub.3)S(O)CH.sub.3                                                                        H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                  H       Me                                                    CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                  H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                  H       OCF.sub.2 H                                           (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                        H       Me                                                    (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                          H       OMe                                                   CH.sub.2 S(O)CF.sub.2 H                                                                         H       OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CH.sub.2 F                                                                CH.sub.3                                                                               OCF.sub.2 H                                           CH.sub.2 S(O)CH.sub.2 CHF.sub.2                                                                 H       Me                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.2 Br                                                               H       OMe                                                   CH.sub.2 S(O)CH.sub.2 CH.sub.2 I                                                                H       OCF.sub.2 H                                           CH.sub.2 S(O)CF.sub.3                                                                           H       Me                                                    CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       OMe                                                   CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                           CH.sub.2 S(O).sub.2 CH.sub.3                                                                    H       Me                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       OMe                                                   (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           OCH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       Me                                                    O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       OMe                                                   O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 C1                                                          H       Me                                                    O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                          H       OMe                                                   O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                           H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 OCF.sub.3                                                                     H       Me                                                    OCH.sub.2 SCH.sub.3                                                                             H       OMe                                                   OCH.sub.2 SCH.sub.3                                                                             H       OCF.sub.2 H                                           OCH.sub.2 SCH.sub.3                                                                             H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OMe                                                   O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OCF.sub.2 H                                           O(CH.sub.2 ).sub.2 SCH.sub.3                                                                    CH.sub.3                                                                               Me                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                     H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                   O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       Me                                                    OCH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OMe                                                   OCH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            H       Me                                                    O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OMe                                                   O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                          H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                          CH.sub.3                                                                               OMe                                                   O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                           H       Me                                                    O(CH.sub.2).sub.2 SCF.sub.3                                                                     H       OMe                                                   OCH.sub.2 S(O)CH.sub.3                                                                          H       OCF.sub.2 H                                           OCH.sub.2 S(O)CH.sub.3                                                                          H       Me                                                    OCH.sub.2 S(O)CH.sub.3                                                                          H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       Me                                                    O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         CH.sub.3                                                                               OCF.sub.2 H                                           O(CH.sub.2).sub. 2 S(O)CH.sub.2 CH.sub.3                                                        H       Me                                                    OCH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       OMe                                                   O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                         H       OCF.sub.2 H                                           OCH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       Me                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                       H       OMe                                                   O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Cl                                                       H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Br                                                       H       Me                                                    O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 I                                                        H       OMe                                                   O(CH.sub.2).sub.2 S(O)CF.sub.3                                                                  H       OCF.sub.2 H                                           OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OMe                                                   OCH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  CH.sub.3                                                                               Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OCF.sub.2 H                                           OCH.sub. 2 S(O).sub.2 CH.sub.2 CH.sub.3                                                         H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                  H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                H       Me                                                    O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Cl                                                H       OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Br                                                H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 I                                                 CH.sub.3                                                                               OMe                                                   O(CH.sub.2).sub.2 S(O).sub.2 CF.sub.3                                                           H       Me                                                    OCH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                H       OMe                                                   OCH.sub.2 S(O).sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 CN                                                                            H       Me                                                    O(CH.sub.2).sub.2 CN                                                                            H       OMe                                                   O(CH.sub.2).sub.2 CN                                                                            H       OCF.sub.2 H                                           OCH.sub.2 CN     H       Me                                                    OCH.sub.2 CN     H       OMe                                                   OCH.sub.2 CN     H       OCF.sub.2 H                                           OCH.sub.2 CN     CH.sub.3                                                                               OCF.sub.2 H                                           OCH(CH.sub.3)CN  H       Me                                                    O(CH.sub.2).sub.2 NH.sub.2                                                                      H       OMe                                                   O(CH.sub.2).sub.2 NH.sub.2                                                                      H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 NH.sub.2                                                                      H       Me                                                    O(CH.sub.2 ).sub.2 NHCH.sub.3                                                                   H       OMe                                                   O(CH.sub.2).sub.2 NHCH.sub.3                                                                    H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 NHCH.sub.3                                                                    H       Me                                                    O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       OMe                                                   O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       OCF.sub.2 H                                           O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                             H       Me                                                    SCH.sub.2 OCH.sub.3                                                                             H       OMe                                                   SCH.sub.2 OCH.sub.3                                                                             H       OCF.sub.2 H                                           SCH.sub.2 OCH.sub.3                                                                             H       Me                                                    SCH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OMe                                                   S(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 OCH.sub.3                                                                     CH.sub.3                                                                               Me                                                    S(CH.sub.2).sub.2 OCH.sub.3                                                                     H       Me                                                    S(CH.sub.2).sub.2 OCH.sub.3                                                                     H       OMe                                                   S(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       Me                                                    SCH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       OMe                                                   S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                          H       Me                                                    S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                          H       OMe                                                   S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                           H       OCF.sub.2 H                                           S(CH.sub.2).sub. 2 OCF.sub.3                                                                    CH.sub.3                                                                               OMe                                                   SCH.sub.2 SCH.sub.3                                                                             H       Me                                                    SCH.sub.2 SCH.sub.3                                                                             H       OMe                                                   SCH.sub.2 SCH.sub.3                                                                             H       OCF.sub.2 H                                           SCH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OMe                                                   S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 SCH.sub.3                                                                     H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                   SCH(CH.sub.3)SCH.sub.3                                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            CH.sub.3                                                                               OCF.sub.2 H                                           SCH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       Me                                                    S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OMe                                                   S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                          H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                          H       Me                                                    S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                           H       OMe                                                   S(CH.sub.2).sub.2 SCF.sub.3                                                                     H       OCF.sub.2 H                                           SCH.sub.2 CN     H       Me                                                    SCH.sub.2 CN     H       OMe                                                   SCH.sub.2 CN     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CN                                                                            H       Me                                                    S(CH.sub.2).sub.2 CN                                                                            H       OMe                                                   S(CH.sub.2).sub.2 CN                                                                            H       OCF.sub.2 H                                           SCH(CH.sub.3)CN  H       Me                                                    SCHF.sub.2       H       OMe                                                   SCHF.sub.2       H       OCF.sub.2 H                                           SCHF.sub.2       CH.sub.3                                                                               Me                                                    SCHF.sub.2       H       Me                                                    SCF.sub.3        H       OMe                                                   SCH.sub.2 CFH.sub.2                                                                             H       OCF.sub.2 H                                           SCH.sub.2 CF.sub.2 H                                                                            H       Me                                                    SCH.sub.2 CF.sub.3                                                                              H       OMe                                                   SCH.sub.2 CF.sub.3                                                                              H       OCF.sub.2 H                                           SCH.sub.2 CF.sub.3                                                                              H       Me                                                    SCH.sub.2 CF.sub.2 H                                                                            H       OMe                                                   S(CH.sub.2).sub.2 CFH.sub.2                                                                     H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CClH.sub.2                                                                    CH.sub.3                                                                               OMe                                                   S(CH.sub.2).sub.2 CIH.sub.2                                                                     H       Me                                                    SCF.sub.2 CF.sub.3                                                                              H       OMe                                                   SCH(CH.sub.3)CF.sub.3                                                                           H       OCF.sub.2 H                                           S(CH.sub.2).sub.2 CCl.sub.3                                                                     H       Me                                                    S(O)CHF.sub.2    H       OMe                                                   S(O)CHF.sub.2    H       OCF.sub.2 H                                           S(O)CHF.sub.2    H       Me                                                    S(O)CF.sub.3     H       OMe                                                   S(O)CH.sub.2 CFH.sub.2                                                                          H       OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.2 H                                                                         CH.sub.3                                                                               OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.3                                                                           H       Me                                                    S(O)CH.sub.2 CF.sub.3                                                                           H       OMe                                                   S(O)CH.sub.2 CF.sub.3                                                                           H       OCF.sub.2 H                                           S(O)CH.sub.2 CF.sub.2 H                                                                         H       Me                                                    S(O)(CH.sub.2).sub.2 CFH.sub.2                                                                  H       OMe                                                   S(O)(CH.sub.2).sub.2 CClH.sub.2                                                                 H       OCF.sub.2 H                                           S(O)(CH.sub.2).sub.2 CIH.sub.2                                                                  H       Me                                                    S(O)CF.sub.2 CF.sub.3                                                                           H       OMe                                                   S(O)CH(CH.sub.3)CF.sub.3                                                                        H       OCF.sub.2 H                                           S(O)(CH.sub.2).sub.2 CCl.sub.3                                                                  H       Me                                                    S(O).sub.2 CHF.sub.2                                                                            H       OMe                                                   S(O).sub.2 CHF.sub.2                                                                            H       OCF.sub.2 H                                           S(O).sub.2 CHF.sub.2                                                                            H       Me                                                    S(O).sub.2 CF.sub.3                                                                             H       OMe                                                   S(O).sub.2 CH.sub.2 CFH.sub.2                                                                   H       OCF.sub.2 H                                           S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                  CH.sub.3                                                                               Me                                                    S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       Me                                                    S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       OMe                                                   S(O).sub.2 CH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                  H       Me                                                    S(O).sub.2 (CH.sub.2).sub.2 CFH.sub.2                                                           H       OMe                                                   S(O).sub.2 (CH.sub.2).sub.2 CClH.sub.2                                                          H       OCF.sub.2 H                                           S(O).sub.2 (CH.sub.2).sub.2 CIH.sub.2                                                           H       Me                                                    S(O).sub.2 CF.sub.2 CF.sub.3                                                                    H       OMe                                                   S(O).sub.2 CH(CH.sub.3)CF.sub.3                                                                 H       OCF.sub.2 H                                           S(O).sub.2 (CH.sub.2).sub.2 CCl.sub.3                                                           CH.sub.3                                                                               OMe                                                   S(O).sub.2 CH.sub.2 Cl                                                                          H       Me                                                    CH═CH.sub.2  H       OMe                                                   CH═CH.sub.2  H       OCF.sub.2 H                                           CH═CH.sub.2  H       Me                                                    CH.sub.2 CH═CH.sub.2                                                                        H       OMe                                                   CH.sub. 2 CH═CH.sub.2                                                                       H       OCF.sub.2 H                                           CH.sub.2 CH═CH.sub.2                                                                        H       Me                                                    CH═CHCH.sub.3                                                                               H       OMe                                                   C(CH.sub.3)═CH.sub.2                                                                        H       OCF.sub.2 H                                           CH═CH.sub.2  CH.sub.3                                                                               OCF.sub.2 H                                           C.tbd.CH         H       Me                                                    C.tbd.CH         H       OMe                                                   C.tbd.CH         H       OCF.sub.2 H                                           CH.sub.2 C.tbd.CH                                                                               H       Me                                                    CH.sub.2 C.tbd.CH                                                                               H       OMe                                                   CH.sub.2 C.tbd.CH                                                                               H       OCF.sub.2 H                                           C.tbd.CCH.sub.3  H       Me                                                    C.tbd.CCH.sub.3  H       OMe                                                   C.tbd.CCH.sub.3  H       OCF.sub.2 H                                           NH.sub.2         H       Me                                                    NH.sub.2         H       OMe                                                   NH.sub.2         H       OCF.sub.2 H                                           NHCH.sub.3       H       Me                                                    NHCH.sub.3       H       OMe                                                   NHCH.sub.3       H       OCF.sub.2 H                                           NHCH.sub.3       CH.sub.3                                                                               Me                                                    N(CH.sub.3).sub.2                                                                               H       Me                                                    N(CH.sub.3).sub.2                                                                               H       OMe                                                   N(CH.sub.3).sub.2                                                                               H       OCF.sub.2 H                                           NHCH.sub.2 CH.sub.3                                                                             H       Me                                                    NHCH.sub.2 CH.sub.3                                                                             H       OMe                                                   NHCH.sub.2 CH.sub.3                                                                             H       OCF.sub.2 H                                           N(CH.sub.3)CH.sub.2 CH.sub.3                                                                    H       Me                                                    N(CH.sub.2 CH.sub.3).sub.2                                                                      H       OMe                                                   NHCH.sub.2 CF.sub.3                                                                             H       OCF.sub.2 H                                           NHCH.sub.2 CF.sub.3                                                                             CH.sub.3                                                                               OMe                                                   NHCH.sub.2 CF.sub.3                                                                             H       Me                                                    NHCH.sub.2 CF.sub.3                                                                             H       OMe                                                   N(CH.sub.3)CH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                           N(CH.sub.3)CH.sub.2 CHF.sub.2                                                                   H       Me                                                    N(CH.sub.3)(CH.sub.2).sub.2 F                                                                   H       OMe                                                   N(CH.sub.3)(CH.sub.2).sub.2 Cl                                                                  H       OCF.sub.2 H                                           N(CH.sub.3)(CH.sub.2).sub.2 I                                                                   H       Me                                                    N(CH.sub.3)(CH.sub.2).sub.2 Br                                                                  H       OMe                                                   NHCF.sub.3       CH.sub.3                                                                               OCF.sub.2 H                                           NHCF.sub.3       H       Me                                                    NH(CH.sub.2).sub.2 F                                                                            H       OMe                                                   N(CH.sub.3)CF.sub.2 H                                                                           H       OCF.sub.2 H                                           NHCF.sub.2 H     H       Me                                                    ______________________________________                                    

                  TABLE VIIIa                                                      ______________________________________                                         R.sub.1 = CH.sub.2 C.tbd.CH                                                    R.sub.2         R       Y         m.p. (°C.)                            ______________________________________                                         Me              H       Me                                                     Me              Me      Me                                                     Me              H       OMe                                                    Me              Me      OMe                                                    Me              H       OCF.sub.2 H                                            Me              Me      OCF.sub.2 H                                            Et              H       Me                                                     Et              Me      Me                                                     Et              H       OMe                                                    Et              Me      OMe                                                    Et              H       OCF.sub.2 H                                            Et              Me      OCF.sub.2 H                                            Pr              H       Me                                                     Pr              Me      Me                                                     Pr              H       OMe                                                    Pr              Me      OMe                                                    Pr              H       OCF.sub.2 H                                            Pr              Me      OCF.sub.2 H                                             .sub.-i-Pr     H       Me                                                      .sub.-i-Pr     Me      Me                                                      .sub.-i-Pr     H       OMe                                                     .sub.-i-Pr     Me      OMe                                                     .sub.-i-Pr     H       OCF.sub.2 H                                             .sub.-i-Pr     Me      OCF.sub.2 H                                            cyclo-Pr        H       Me                                                     cyclo-Pr        Me      Me                                                     cyclo-Pr        H       OMe                                                    cyclo-Pr        Me      OMe                                                    cyclo-Pr        H       OCF.sub.2 H                                            cyclo-Pr        Me      OCF.sub.2 H                                            OMe             H       Me                                                     OMe             Me      Me                                                     OMe             H       OMe                                                    OMe             Me      OMe                                                    OMe             H       OCF.sub.2 H                                            OMe             Me      OCF.sub.2 H                                            OEt             H       Me                                                     OEt             Me      Me                                                     OEt             H       OMe                                                    OEt             Me      OMe                                                    OEt             H       OCF.sub.2 H                                            OEt             Me      OCF.sub.2 H                                            O-- -n-Pr       H       Me                                                     O-- -n-Pr       Me      Me                                                     O-- -n-Pr       H       OMe                                                    O-- -n-Pr       Me      OMe                                                    O-- -n-Pr       H       OCF.sub.2 H                                            O-- -n-Pr       Me      OCF.sub.2 H                                            O-- .sub.-i-Pr  H       Me                                                     O-- .sub.-i-Pr  Me      Me                                                     O-- .sub.-i-Pr  H       OMe                                                    O-- .sub.-i-Pr  Me      OMe                                                    O-- .sub.-i-Pr  H       OCF.sub.2 H                                            O-- .sub.-i-Pr  Me      OCF.sub.2 H                                            SMe             H       Me                                                     SMe             Me      Me                                                     SMe             H       OMe                                                    SMe             Me      OMe                                                    SMe             H       OCF.sub.2 H                                            SMe             Me      OCF.sub.2 H                                            SEt             H       Me                                                     SEt             Me      Me                                                     SEt             H       OMe                                                    SEt             Me      OMe                                                    SEt             H       OCF.sub.2 H                                            SEt             Me      OCF.sub.2 H                                            S-- -n-Pr       H       Me                                                     S-- -n-Pr       Me      Me                                                     S-- -n-Pr       H       OMe                                                    S-- -n-Pr       Me      OMe                                                    S-- -n-Pr       H       OCF.sub.2 H                                            S-- -n-Pr       Me      OCF.sub.2 H                                            S-- .sub.-i-Pr  H       Me                                                     S-- .sub.-i-Pr  Me      Me                                                     S-- .sub.-i-Pr  H       OMe                                                    S-- .sub.-i-Pr  Me      OMe                                                    S-- .sub.-i-Pr  H       OCF.sub.2 H                                            S-- .sub.-i-Pr  Me      OCF.sub.2 H                                            O--allyl        H       Me                                                     O--allyl        Me      Me                                                     O--allyl        H       OMe                                                    O--allyl        Me      OMe                                                    O--allyl        H       OCF.sub.2 H                                            O--allyl        Me      OCF.sub.2 H                                            O--propargyl    H       Me                                                     O--propargyl    Me      Me                                                     O--propargyl    H       OMe                                                    O--propargyl    Me      OMe                                                    O--propargyl    H       OCF.sub.2 H                                            O--propargyl    Me      OCF.sub.2 H                                            CH.sub.2 F      H       Me                                                     CH.sub.2 F      Me      Me                                                     CH.sub.2 F      H       OMe                                                    CH.sub.2 F      Me      OMe                                                    CH.sub.2 F      H       OCF.sub.2 H                                            CH.sub.2 F      Me      OCF.sub.2 H                                            CHF.sub.2       H       Me                                                     CHF.sub.2       Me      Me                                                     CHF.sub.2       H       OMe                                                    CHF.sub.2       Me      OMe                                                    CHF.sub.2       H       OCF.sub.2 H                                            CHF.sub.2       Me      OCF.sub.2 H                                            CF.sub.3        H       Me                                                     CF.sub.3        Me      Me                                                     CF.sub.3        H       OMe                                                    CF.sub.3        Me      OMe                                                    CF.sub.3        H       OCF.sub.2 H                                            CF.sub.3        Me      OCF.sub.2 H                                            CH.sub.2 Cl     H       Me                                                     CH.sub.2 Cl     Me      Me                                                     CH.sub.2 Cl     H       OMe                                                    CH.sub.2 Cl     Me      OMe                                                    CH.sub.2 Cl     H       OCF.sub.2 H                                            CH.sub.2 Cl     Me      OCF.sub.2 H                                            CHCl.sub.2      H       Me                                                     CHCl.sub.2      Me      Me                                                     CHCl.sub.2      H       OMe                                                    CHCl.sub.2      Me      OMe                                                    CHCl.sub.2      H       OCF.sub.2 H                                            CHCl.sub.2      Me      OCF.sub.2 H                                            CCl.sub. 3      H       Me                                                     CCl.sub.3       Me      Me                                                     CCl.sub.3       H       OMe                                                    CCl.sub.3       Me      OMe                                                    CCl.sub.3       H       OCF.sub.2 H                                            CCl.sub.3       Me      OCF.sub.2 H                                            CHFCH.sub.3     H       Me                                                     CHFCH.sub.3     Me      Me                                                     CHFCH.sub.3     H       OMe                                                    CHFCH.sub.3     Me      OMe                                                    CHFCH.sub.3     H       OCF.sub.2 H                                            CHFCH.sub.3     Me      OCF.sub.2 H                                            CF.sub.2 CH.sub.3                                                                              H       Me                                                     CF.sub.2 CH.sub.3                                                                              Me      Me                                                     CF.sub.2 CH.sub.3                                                                              H       OMe                                                    CF.sub.2 CH.sub.3                                                                              Me      OMe                                                    CF.sub.2 CH.sub.3                                                                              H       OCF.sub.2 H                                            CF.sub.2 CH.sub.3                                                                              Me      OCF.sub.2 H                                            CH.sub.2 CH.sub.2 F                                                                            H       Me                                                     CH.sub.2 CH.sub.2 F                                                                            Me      Me                                                     CH.sub.2 CH.sub.2 F                                                                            H       OMe                                                    CH.sub.2 CH.sub.2 F                                                                            Me      OMe                                                    CH.sub.2 CH.sub.2 F                                                                            H       OCF.sub.2 H                                            CH.sub.2 CH.sub.2 F                                                                            Me      OCF.sub.2 H                                            CH.sub.2 CHF.sub.2                                                                             H       Me                                                     CH.sub.2 CHF.sub.2                                                                             Me      Me                                                     CH.sub.2 CHF.sub.2                                                                             H       OMe                                                    CH.sub.2 CHF.sub.2                                                                             Me      OMe                                                    CH.sub.2 CHF.sub.2                                                                             H       OCF.sub.2 H                                            CH.sub.2 CHF.sub.2                                                                             Me      OCF.sub.2 H                                            CH.sub.2 CF.sub.3                                                                              H       Me                                                     CH.sub.2 CF.sub.3                                                                              Me      Me                                                     CH.sub.2 CF.sub.3                                                                              H       OMe                                                    CH.sub.2 CF.sub.3                                                                              Me      OMe                                                    CH.sub.2 CF.sub.3                                                                              H       OCF.sub.2 H                                            CH.sub.2 CF.sub.3                                                                              Me      OCF.sub.2 H                                            CHClCH.sub.3    H       Me                                                     CHClCH.sub.3    Me      Me                                                     CHClCH.sub.3    H       OMe                                                    CHClCH.sub.3    Me      OMe                                                    CHClCH.sub.3    H       OCF.sub.2 H                                            CHClCH.sub.3    Me      OCF.sub.2 H                                            CH.sub.2 OCH.sub.3                                                                             H       Me                                                     CH.sub.2 OCH.sub.3                                                                             Me      Me                                                     CH.sub.2 OCH.sub.3                                                                             H       OMe                                                    CH.sub.2 OCH.sub.3                                                                             Me      OMe                                                    CH.sub.2 OCH.sub.3                                                                             H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.3                                                                             Me      OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.3                                                                     H       Me                                                     (CH.sub.2).sub.2 OCH.sub.3                                                                     Me      Me                                                     (CH.sub.2).sub.2 OCH.sub.3                                                                     H       OMe                                                    (CH.sub.2).sub.2 OCH.sub.3                                                                     Me      OMe                                                    (CH.sub.2).sub.2 OCH.sub.3                                                                     H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.3                                                                     Me      OCF.sub.2 H                                            CH(OCH.sub.3)CH.sub.3                                                                          H       Me                                                     CH(OCH.sub.3)CH.sub.3                                                                          Me      Me                                                     CH(OCH.sub.3)CH.sub.3                                                                          H       OMe                                                    CH(OCH.sub.3)CH.sub.3                                                                          Me      OMe                                                    CH(OCH.sub.3)CH.sub.3                                                                          H       OCF.sub.2 H                                            CH(OCH.sub.3)CH.sub.3                                                                          Me      OCF.sub.2 H                                            CH.sub.2 SCH.sub.3                                                                             H       Me                                                     CH.sub.2 SCH.sub.3                                                                             Me      Me                                                     CH.sub.2 SCH.sub.3                                                                             H       OMe                                                    CH.sub.2 SCH.sub.3                                                                             Me      OMe                                                    CH.sub.2 SCH.sub.3                                                                             H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.3                                                                             Me      OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.3                                                                     H       Me                                                     (CH.sub.2).sub.2 SCH.sub.3                                                                     Me      Me                                                     (CH.sub.2).sub.2 SCH.sub.3                                                                     H       OMe                                                    (CH.sub.2).sub.2 SCH.sub.3                                                                     Me      OMe                                                    (CH.sub.2).sub.2 SCH.sub.3                                                                     H       OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.3                                                                     Me      OCF.sub.2 H                                            CH(SCH.sub.3)CH.sub.3                                                                          H       Me                                                     CH(SCH.sub.3)CH.sub.3                                                                          Me      Me                                                     CH(SCH.sub.3)CH.sub.3                                                                          H       OMe                                                    CH(SCH.sub.3)CH.sub.3                                                                          Me      OMe                                                    CH(SCH.sub.3)CH.sub.3                                                                          H       OCF.sub.2 H                                            CH(SCH.sub.3)CH.sub.3                                                                          Me      OCF.sub.2 H                                            OCF.sub.2 H     H       Me                                                     OCF.sub.2 H     Me      Me                                                     OCF.sub.2 H     H       OMe                                                    OCF.sub.2 H     Me      OMe                                                    OCF.sub.2 H     H       OCF.sub.2 H                                            OCF.sub.2 H     Me      OCF.sub.2 H                                            OCH.sub.2 CH.sub.2 F                                                                           H       Me                                                     OCH.sub.2 CH.sub.2 F                                                                           Me      Me                                                     OCH.sub.2 CH.sub.2 F                                                                           H       OMe                                                    OCH.sub.2 CH.sub.2 F                                                                           Me      OMe                                                    OCH.sub.2 CH.sub.2 F                                                                           H       OCF.sub.2 H                                            OCH.sub.2 CH.sub.2 F                                                                           Me      OCF.sub.2 H                                            OCH.sub.2 CHF.sub.2                                                                            H       Me                                                     OCH.sub.2 CHF.sub.2                                                                            Me      Me                                                     OCH.sub.2 CHF.sub.2                                                                            H       OMe                                                    OCH.sub.2 CHF.sub.2                                                                            Me      OMe                                                    OCH.sub.2 CHF.sub.2                                                                            H       OCF.sub.2 H                                            OCH.sub.2 CHF.sub.2                                                                            Me      OCF.sub.2 H                                            OCH.sub.2 CF.sub.3                                                                             H       Me                                                     OCH.sub.2 CF.sub.3                                                                             Me      Me                                                     OCH.sub.2 CF.sub.3                                                                             H       OMe                                                    OCH.sub.2 CF.sub.3                                                                             Me      OMe                                                    OCH.sub.2 CF.sub.3                                                                             H       OCF.sub.2 H                                            OCH.sub.2 CF.sub.3                                                                             Me      OCF.sub.2 H                                            O(CH.sub.2).sub.2 Cl                                                                           H       Me                                                     O(CH.sub.2).sub.2 Cl                                                                           Me      Me                                                     O(CH.sub.2).sub.2 Cl                                                                           H       OMe                                                    O(CH.sub.2).sub.2 Cl                                                                           Me      OMe                                                    O(CH.sub.2).sub.2 Cl                                                                           H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 Cl                                                                           Me      OCF.sub.2 H                                            S(O)Me          H       Me                                                     S(O)Me          Me      Me                                                     S(O)Me          H       OMe                                                    S(O)Me          Me      OMe                                                    S(O)Me          H       OCF.sub.2 H                                            S(O)Me          Me      OCF.sub.2 H                                            S(O)Et          H       Me                                                     S(O)Et          Me      Me                                                     S(O)Et          H       OMe                                                    S(O)Et          Me      OMe                                                    S(O)Et          H       OCF.sub.2 H                                            S(O)Et          Me      OCF.sub.2 H                                            S(O)-- -n-Pr    H       Me                                                     S(O)-- -n-Pr    Me      Me                                                     S(O)-- -n-Pr    H       OMe                                                    S(O)-- -n-Pr    Me      OMe                                                    S(O)-- -n-Pr    H       OCF.sub.2 H                                            S(O)-- -n-Pr    Me      OCF.sub.2 H                                            S(O)-- .sub.-i-Pr                                                                              H       Me                                                     S(O)-- .sub.-i-Pr                                                                              Me      Me                                                     S(O)-- .sub.-i-Pr                                                                              H       OMe                                                    S(O)-- .sub.-i-Pr                                                                              Me      Me                                                     S(O)-- .sub.-i-Pr                                                                              H       OCF.sub.2 H                                            S(O)-- .sub.-i-Pr                                                                              Me      OCF.sub.2 H                                            SO.sub.2 Me     H       Me                                                     SO.sub.2 Me     Me      Me                                                     SO.sub.2 Me     H       OMe                                                    SO.sub.2 Me     Me      OMe                                                    SO.sub. 2 Me    H       OCF.sub.2 H                                            SO.sub.2 Me     Me      OCF.sub.2 H                                            SO.sub.2 Et     H       Me                                                     SO.sub.2 Et     Me      Me                                                     SO.sub.2 Et     H       OMe                                                    SO.sub.2 Et     Me      OMe                                                    SO.sub.2 Et     H       OCF.sub.2 H                                            SO.sub.2 Et     Me      OCF.sub.2 H                                            SO.sub.2 -- -n-Pr                                                                              H       Me                                                     SO.sub.2 -- -n-Pr                                                                              Me      Me                                                     SO.sub.2 -- -n-Pr                                                                              H       OMe                                                    SO.sub.2 -- -n-Pr                                                                              Me      OMe                                                    SO.sub.2 -- -n-Pr                                                                              H       OCF.sub.2 H                                            SO.sub.2 -- -n-Pr                                                                              Me      OCF.sub.2 H                                            SO.sub.2 -- .sub.-i-Pr                                                                         H       Me                                                     SO.sub.2 -- .sub.-i-Pr                                                                         Me      Me                                                     SO.sub.2 -- .sub.-i-Pr                                                                         H       OMe                                                    SO.sub.2 -- .sub.-i-Pr                                                                         Me      OMe                                                    SO.sub.2 -- .sub.-i-Pr                                                                         H       OCF.sub.2 H                                            SO.sub.2 -- .sub.-i-Pr                                                                         Me      OCF.sub.2 H                                            S--allyl        H       Me                                                     S--allyl        Me      Me                                                     S--allyl        H       OMe                                                    S--allyl        Me      OMe                                                    S--allyl        H       OCF.sub.2 H                                            S--allyl        Me      OCF.sub.2 H                                            S(O)allyl       H       Me                                                     S(O)allyl       Me      Me                                                     S(O)allyl       H       OMe                                                    S(O)allyl       Me      OMe                                                    S(O)allyl       H       OCF.sub.2 H                                            S(O)allyl       Me      OCF.sub.2 H                                            SO.sub.2 allyl  H       Me                                                     SO.sub.2 allyl  Me      Me                                                     SO.sub.2 allyl  H       OMe                                                    SO.sub.2 allyl  Me      OMe                                                    SO.sub.2 allyl  H       OCF.sub.2 H                                            SO.sub.2 allyl  Me      OCF.sub.2 H                                            S--propargyl    H       Me                                                     S--propargyl    Me      Me                                                     S--propargyl    H       OMe                                                    S--propargyl    Me      OMe                                                    S--propargyl    H       OCF.sub.2 H                                            S--propargyl    Me      OCF.sub.2 H                                            S(O)propargyl   H       Me                                                     S(O)propargyl   Me      Me                                                     S(O)propargyl   H       OMe                                                    S(O)propargyl   Me      OMe                                                    S(O)propargyl   H       OCF.sub.2 H                                            S(O)propargyl   Me      OCF.sub.2 H                                            SO.sub.2 propargyl                                                                             H       Me                                                     SO.sub.2 propargyl                                                                             Me      Me                                                     SO.sub.2 propargyl                                                                             H       OMe                                                    SO.sub.2 propargyl                                                                             Me      OMe                                                    SO.sub.2 propargyl                                                                             H       OCF.sub.2 H                                            SO.sub.2 propargyl                                                                             Me      OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       Me                                                     CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OMe                                                    CH.sub.2 OCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       Me                                                     (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OMe                                                    (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                            CH.sub.3                                                                               Me                                                     CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       Me                                                     CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH(CH.sub.3)OCH.sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       Me                                                     CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       OMe                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                            (CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                          H       Me                                                     (CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                            H       OMe                                                    CH.sub.2 OCF.sub.2 H                                                                           H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                  CH.sub.3                                                                               OMe                                                    CH.sub.2 OCH.sub.2 CHF.sub.2                                                                   H       Me                                                     CH.sub.2 OCH.sub.2 CH.sub.2 Br                                                                 H       OMe                                                    CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                 H       OCF.sub.2 H                                            CH.sub.2 OCH.sub.2 CH.sub.2 I                                                                  H       Me                                                     CH.sub.2 OCF.sub.3                                                                             H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       Me                                                     CH.sub.2 SCH.sub.2 CH.sub.3                                                                    H       OMe                                                    (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OCF.sub.2 H                                            (CH.sub.2 ).sub.2 SCH.sub.2 CH.sub.3                                                           CH.sub.3                                                                               OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       Me                                                     (CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                            H       OMe                                                    CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                            CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       Me                                                     CH(CH.sub.3)SCH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       Me                                                     CH.sub.2 SCH.sub.2 CF.sub.3                                                                    H       OMe                                                    (CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                          H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                          H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                  H       OMe                                                    CH(CH.sub.3)S(O).sub.2 CH.sub.3                                                                H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          CH.sub.3                                                                               Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                          H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                                H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CF.sub.2 CF.sub.3                                                  H       OMe                                                    CH.sub.2 S(O).sub.2 CF.sub.2 H                                                                 H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 F                                                        H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 CHF.sub.2                                                         H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 Br                                                       H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.2 I                                                        CH.sub.3                                                                               OMe                                                    CH.sub.2 S(O).sub.2 CF.sub.3                                                                   H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                                H       OMe                                                    OCH.sub.2 OCH.sub.3                                                                            H       OCF.sub.2 H                                            OCH.sub.2 OCH.sub.3                                                                            H       Me                                                     OCH.sub.2 OCH.sub.3                                                                            H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           CH.sub.3                                                                               OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OMe                                                    OCH.sub.2 OCH.sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                            (CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                            H       Me                                                     CH.sub.2 SCF.sub.2 H                                                                           H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.2 F                                                                  H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CHF.sub.2                                                                   H       Me                                                     CH.sub.2 SCH.sub.2 CH.sub.2 Br                                                                 H       OMe                                                    CH.sub.2 SCH.sub.2 CH.sub.2 Cl                                                                 H       OCF.sub.2 H                                            CH.sub.2 SCH.sub.2 CH.sub.2 I                                                                  CH.sub.3                                                                               Me                                                     CH.sub.2 SCF.sub.3                                                                             H       Me                                                     CH.sub.2 S(O)CH.sub.3                                                                          H       OMe                                                    CH.sub.2 S(O)CH.sub.3                                                                          H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.3                                                                          H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OMe                                                    (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O)CH.sub.3                                                                  H       Me                                                     CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       OMe                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 CH.sub.3                                                                               OMe                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                 H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                         H       OMe                                                    CH(CH.sub.3)S(O)CH.sub.3                                                                       H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       Me                                                     CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       OMe                                                    CH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                 H       OCF.sub.2 H                                            (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                       H       Me                                                     (CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                         H       OMe                                                    CH.sub.2 S(O)CF.sub.2 H                                                                        H       OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CH.sub.2 F                                                               CH.sub.3                                                                               OCF.sub.2 H                                            CH.sub.2 S(O)CH.sub.2 CHF.sub.2                                                                H       Me                                                     CH.sub.2 S(O)CH.sub.2 CH.sub.2 Br                                                              H       OMe                                                    CH.sub.2 S(O)CH.sub.2 CH.sub.2 I                                                               H       OCF.sub.2 H                                            CH.sub.2 S(O)CF.sub.3                                                                          H       Me                                                     CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OMe                                                    CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       OCF.sub.2 H                                            CH.sub.2 S(O).sub.2 CH.sub.3                                                                   H       Me                                                     (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OMe                                                    (CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            OCH.sub.2 OCH.sub.2 CF.sub.3                                                                   H       Me                                                     O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                           H       OMe                                                    O(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                         H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                         H       Me                                                     O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                         H       OMe                                                    O(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                          H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 OCF.sub.3                                                                    H       Me                                                     OCH.sub.2 SCH.sub.3                                                                            H       OMe                                                    OCH.sub.2 SCH.sub.3                                                                            H       OCF.sub.2 H                                            OCH.sub.2 SCH.sub.3                                                                            H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OMe                                                    O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.3                                                                    CH.sub.3                                                                               Me                                                     O(CH.sub.2).sub.2 SCH.sub.3                                                                    H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OMe                                                    O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       Me                                                     OCH.sub.2 SCH.sub.2 CH.sub.3                                                                   H       OMe                                                    OCH.sub.2 SCH.sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                           H       Me                                                     O(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                         H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                         CH.sub.3                                                                               OMe                                                    O(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                          H       Me                                                     O(CH.sub.2).sub.2 SCF.sub.3                                                                    H       OMe                                                    OCH.sub.2 S(O)CH.sub.3                                                                         H       OCF.sub.2 H                                            OCH.sub.2 S(O)CH.sub.3                                                                         H       Me                                                     OCH.sub.2 S(O)CH.sub.3                                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                 H       OCF.sub.2 H                                            O(CH.sub.2 ).sub.2 S(O)CH.sub.3                                                                H       Me                                                     O(CH.sub.2).sub.2 S(O)CH.sub.3                                                                 H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        CH.sub.3                                                                               OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)CH.sub.2 CH.sub.3                                                        H       Me                                                     OCH.sub.2 S(O)CH.sub.2 CH.sub.3                                                                H       OMe                                                    O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.3                                                        H       OCF.sub.2 H                                            OCH.sub.2 S(O)CH.sub.2 CF.sub.3                                                                H       Me                                                     O(CH.sub.2).sub.2 S(O)CH.sub.2 CF.sub.2 H                                                      H       OMe                                                    O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Cl                                                      H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 Br                                                      H       Me                                                     O(CH.sub.2).sub.2 S(O)(CH.sub.2).sub.2 I                                                       H       OMe                                                    O(CH.sub.2).sub.2 S(O)CF.sub.3                                                                 H       OCF.sub.2 H                                            OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       OMe                                                    OCH.sub.2 S(O).sub.2 CH.sub.3                                                                  H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.3                                                          H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub. 3                                                CH.sub.3                                                                               Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                 H       OCF.sub.2 H                                            OCH.sub.2 S(O).sub.2 CH.sub.2 CH.sub.3                                                         H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                         H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.3                                                 H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 CH.sub.2 CF.sub.2 H                                               H       Me                                                     O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Cl                                               H       OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 Br                                               H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 S(O).sub.2 (CH.sub.2).sub.2 I                                                CH.sub.3                                                                               OMe                                                    O(CH.sub.2).sub.2 S(O).sub.2 CF.sub.3                                                          H       Me                                                     OCH.sub.2 S(O).sub.2 CH.sub.2 Cl                                                               H       OMe                                                    OCH.sub.2 S(O).sub.2 CF.sub.3                                                                  H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 CN                                                                           H       Me                                                     O(CH.sub.2).sub.2 CN                                                                           H       OMe                                                    O(CH.sub.2).sub.2 CN                                                                           H       OCF.sub.2 H                                            OCH.sub.2 CN    H       Me                                                     OCH.sub.2 CN    H       OMe                                                    OCH.sub.2 CN    H       OCF.sub.2 H                                            OCH.sub.2 CN    CH.sub.3                                                                               OCF.sub.2 H                                            OCH(CH.sub.3)CN H       Me                                                     O(CH.sub.2).sub.2 NH.sub.2                                                                     H       OMe                                                    O(CH.sub.2).sub.2 NH.sub.2                                                                     H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 NH.sub.2                                                                     H       Me                                                     O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       OMe                                                    O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 NHCH.sub.3                                                                   H       Me                                                     O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       OMe                                                    O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       OCF.sub.2 H                                            O(CH.sub.2).sub.2 N(CH.sub.3).sub.2                                                            H       Me                                                     SCH.sub.2 OCH.sub.3                                                                            H       OMe                                                    SCH.sub.2 OCH.sub.3                                                                            H       OCF.sub.2 H                                            SCH.sub.2 OCH.sub.3                                                                            H       Me                                                     SCH.sub.2 OCH.sub.2 CH.sub.3                                                                   H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCH.sub.3                                                                    CH.sub.3                                                                               Me                                                     S(CH.sub.2).sub.2 OCH.sub.3                                                                    H       Me                                                     S(CH.sub.2).sub.2 OCH.sub.3                                                                    H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub.2 CH.sub.3                                                           H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.3                                                           H       Me                                                     SCH.sub.2 OCH.sub.2 CF.sub.3                                                                   H       OMe                                                    S(CH.sub.2).sub.2 OCH.sub.2 CF.sub.2 H                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Cl                                                         H       Me                                                     S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 Br                                                         H       Ome                                                    S(CH.sub.2).sub.2 O(CH.sub.2).sub.2 I                                                          H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 OCF.sub.3                                                                    CH.sub.3                                                                               OMe                                                    SCH.sub.2 SCH.sub.3                                                                            H       Me                                                     SCH.sub.2 SCH.sub.3                                                                            H       OMe                                                    SCH.sub.2 SCH.sub.3                                                                            H       OCF.sub.2 H                                            SCH.sub.2 SCH.sub.2 CH.sub.3                                                                   H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OMe                                                    S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 SCH.sub.3                                                                    H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.2 CH.sub.3                                                           H       OMe                                                    SCH(CH.sub.3)SCH.sub.3                                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.3                                                           CH.sub.3                                                                               OCF.sub.2 H                                            SCH.sub.2 SCH.sub.2 CF.sub.3                                                                   H       Me                                                     S(CH.sub.2).sub.2 SCH.sub.2 CF.sub.2 H                                                         H       OMe                                                    S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Cl                                                         H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 Br                                                         H       Me                                                     S(CH.sub.2).sub.2 S(CH.sub.2).sub.2 I                                                          H       OMe                                                    S(CH.sub.2).sub.2 SCF.sub.3                                                                    H       OCF.sub.2 H                                            SCH.sub.2 CN    H       Me                                                     SCH.sub.2 CN    H       OMe                                                    SCH.sub.2 CN    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CN                                                                           H       Me                                                     S(CH.sub.2).sub.2 CN                                                                           H       OMe                                                    S(CH.sub.2).sub.2 CN                                                                           H       OCF.sub.2 H                                            SCH(CH.sub.3)CN H       Me                                                     SCHF.sub.2      H       OMe                                                    SCHF.sub.2      H       OCF.sub.2 H                                            SCHF.sub.2      CH.sub.3                                                                               Me                                                     SCHF.sub.2      H       Me                                                     SCF.sub.3       H       OMe                                                    SCH.sub.2 CFH.sub.2                                                                            H       OCF.sub.2 H                                            SCH.sub.2 CF.sub.2 H                                                                           H       Me                                                     SCH.sub.2 CF.sub.3                                                                             H       OMe                                                    SCH.sub.2 CF.sub.3                                                                             H       OCF.sub.2 H                                            SCH.sub.2 CF.sub.3                                                                             H       Me                                                     SCH.sub.2 CF.sub.2 H                                                                           H       OMe                                                    S(CH.sub.2).sub.2 CFH.sub.2                                                                    H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CClH.sub.2                                                                   CH.sub.3                                                                               OMe                                                    S(CH.sub.2).sub.2 CIH.sub.2                                                                    H       Me                                                     SCF.sub.2 CF.sub.3                                                                             H       OMe                                                    SCH(CH.sub.3)CF.sub.3                                                                          H       OCF.sub.2 H                                            S(CH.sub.2).sub.2 CCl.sub.3                                                                    H       Me                                                     S(O)CHF.sub.2   H       OMe                                                    S(O)CHF.sub.2   H       OCF.sub.2 H                                            S(O)CHF.sub.2   H       Me                                                     S(O)CF.sub.3    H       OMe                                                    S(O)CH.sub.2 CFH.sub.2                                                                         H       OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.2 H                                                                        CH.sub.3                                                                               OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.3                                                                          H       Me                                                     S(O)CH.sub.2 CF.sub.3                                                                          H       OMe                                                    S(O)CH.sub. 2 CF.sub.3                                                                         H       OCF.sub.2 H                                            S(O)CH.sub.2 CF.sub.2 H                                                                        H       Me                                                     S(O)(CH.sub.2).sub.2 CFH.sub.2                                                                 H       OMe                                                    S(O)(CH.sub.2).sub.2 CClH.sub.2                                                                H       OCF.sub.2 H                                            S(O)(CH.sub.2).sub.2 CIH.sub.2                                                                 H       Me                                                     S(O)CF.sub.2 CF.sub.3                                                                          H       OMe                                                    S(O)CH(CH.sub.3)CF.sub.3                                                                       H       OCF.sub.2 H                                            S(O)(CH.sub.2).sub.2 CCl.sub.3                                                                 H       Me                                                     S(O).sub.2 CHF.sub.2                                                                           H       OMe                                                    S(O).sub.2 CHF.sub.2                                                                           H       OCF.sub.2 H                                            S(O).sub.2 CHF.sub.2                                                                           H       Me                                                     S(O).sub.2 CF.sub.3                                                                            H       OMe                                                    S(O).sub.2 CH.sub.2 CFH.sub.2                                                                  H       OCF.sub.2 H                                            S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                 CH.sub.3                                                                               Me                                                     S(O).sub.2 CH.sub.2 CF.sub.3                                                                   H       Me                                                     S(O).sub.2 CH.sub.2 CF.sub.3                                                                   H       OMe                                                    S(O).sub.2 CH.sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                            S(O).sub.2 CH.sub.2 CF.sub.2 H                                                                 H       Me                                                     S(O).sub.2 (CH.sub.2).sub.2 CFH.sub.2                                                          H       OMe                                                    S(O).sub.2 (CH.sub.2).sub.2 CClH.sub.2                                                         H       OCF.sub.2 H                                            S(O).sub.2 (CH.sub.2).sub.2 CIH.sub.2                                                          H       Me                                                     S(O).sub.2 CF.sub.2 CF.sub.3                                                                   H       OMe                                                    S(O).sub.2 CH(CH.sub.3)CF.sub.3                                                                H       OCF.sub.2 H                                            S(O).sub.2 (CH.sub.2).sub.2 CCl.sub. 3                                                         CH.sub.3                                                                               OMe                                                    S(O).sub.2 CH.sub.2 Cl                                                                         H       Me                                                     CH═CH.sub.2 H       OMe                                                    CH═CH.sub.2 H       OCF.sub.2 H                                            CH═CH.sub.2 H       Me                                                     CH.sub.2 CH═CH.sub.2                                                                       H       OMe                                                    CH.sub.2 CH═CH.sub.2                                                                       H       OCF.sub.2 H                                            CH.sub.2 CH═CH.sub.2                                                                       H       Me                                                     CH═CHCH.sub.3                                                                              H       OMe                                                    C(CH.sub.3)═CH.sub.2                                                                       H       OCF.sub.2 H                                            CH═CH.sub.2 CH.sub.3                                                                               OCF.sub.2 H                                            C.tbd.CH        H       Me                                                     C.tbd.CH        H       OMe                                                    C.tbd.CH        H       OCF.sub.2 H                                            CH.sub.2 C.tbd.CH                                                                              H       Me                                                     CH.sub.2 C.tbd.CH                                                                              H       OMe                                                    CH.sub.2 C.tbd.CH                                                                              H       OCF.sub.2 H                                            C.tbd.CCH.sub.3 H       Me                                                     C.tbd.CCH.sub.3 H       OMe                                                    C.tbd.CCH.sub.3 H       OCF.sub.2 H                                            NH.sub.2        H       Me                                                     NH.sub.2        H       OMe                                                    NH.sub.2        H       OCF.sub.2 H                                            NHCH.sub.3      H       Me                                                     NHCH.sub.3      H       OMe                                                    NHCH.sub.3      H       OCF.sub.2 H                                            NHCH.sub.3      CH.sub.3                                                                               Me                                                     N(CH.sub.3).sub.2                                                                              H       Me                                                     N(CH.sub.3).sub.2                                                                              H       OMe                                                    N(CH.sub.3).sub.2                                                                              H       OCF.sub.2 H                                            NHCH.sub.2 CH.sub.3                                                                            H       Me                                                     NHCH.sub.2 CH.sub.3                                                                            H       OMe                                                    NHCH.sub.2 CH.sub.3                                                                            H       OCF.sub.2 H                                            N(CH.sub.3)CH.sub. 2 CH.sub.3                                                                  H       Me                                                     N(CH.sub.2 CH.sub.3).sub.2                                                                     H       OMe                                                    NHCH.sub.2 CF.sub.3                                                                            H       OCF.sub.2 H                                            NHCH.sub.2 CF.sub.3                                                                            CH.sub.3                                                                               OMe                                                    NHCH.sub.2 CF.sub.3                                                                            H       Me                                                     NHCH.sub.2 CF.sub.3                                                                            H       OMe                                                    N(CH.sub.3)CH.sub.2 CF.sub.3                                                                   H       OCF.sub.2 H                                            N(CH.sub.3)CH.sub.2 CHF.sub.2                                                                  H       Me                                                     N(CH.sub.3)(CH.sub.2).sub.2 F                                                                  H       OMe                                                    N(CH.sub.3)(CH.sub.2).sub.2 Cl                                                                 H       OCF.sub.2 H                                            N(CH.sub.3)(CH.sub.2).sub.2 I                                                                  H       Me                                                     N(CH.sub.3)(CH.sub.2).sub.2 Br                                                                 H       OMe                                                    NHCF.sub.3      CH.sub.3                                                                               OCF.sub.2 H                                            NHCF.sub.3      H       Me                                                     NH(CH.sub.2).sub.2 F                                                                           H       OMe                                                    N(CH.sub.3)CF.sub.2 H                                                                          H       OCF.sub.2 H                                            NHCF.sub.2 H    H       Me                                                     ______________________________________                                    

FORMULATIONS

Useful formulations of the compounds of Formula I can be prepared in conventional ways. They include dusts, granules, pellets, solutions, suspensions, emulsions, wettable powders, emulsifiable concentrates and the like. Many of these may be applied directly. Sprayable formulations can be extended in suitable media and used at spray volumes of from a few liters to several hundred liters per hectare. High strength compositions are primarily used as intermediates for further formulation. The formulations, broadly, contain about 0.1% to 99% by weight of active ingredient(s) and at least one of (a) about 0.1% to 20% surfactant(s) and (b) about 1% to 99.9% solid or liquid inert diluent(s). More specifically, they will contain these ingredients in the following approximate proportions:

                  TABLE IX                                                         ______________________________________                                                     Active  Weight Percent*                                                        Ingredient                                                                             Diluent(s)                                                                               Surfactant(s)                                    ______________________________________                                         Wettable Powders                                                                             20-90     0-74      1-10                                         Oil Suspensions,                                                                             3-50      40-95     0-15                                         Emulsions, Solutions,                                                          (including Emulsifiable                                                        Concentrates)                                                                  Aqueous Suspension                                                                           10-50     40-84     1-20                                         Dusts         1-25      70-99     0-5                                          Granules and Pellets                                                                         0.1-95    5-99.9    0-15                                         High Strength 90-99     0-10      0-2                                          Compositions                                                                   ______________________________________                                          *Active ingredient plus at least one of a Surfactant or a Diluent equals       100 weight percent.                                                      

Lower or higher levels of active ingredient can, of course, be present depending on the intended use and the physical properties of the compound. Higher ratios of surfactant to active ingredient are sometimes desirable, and are achieved by incorporation into the formulation or by tank mixing.

Typical solid diluents are described in Watkins, et al., "Handbook of Insecticide Dust Diluents and Carriers", 2nd Ed., Dorland Books, Caldwell, N.J., but other solids, either mined or manufactured, may be used. The more absorptive diluents are preferred for wettable powders and the denser ones for dusts. Typical liquid diluents and solvents are described in Marsden, "Solvents Guide," 2nd Ed., Interscience, New York, 1950. Solubility under 0.1% is preferred for suspension concentrates; solution concentrates are preferably stable against phase separation at 0° C. "McCutcheon's Detergents and Emulsifiers Annual", MC Publishing Corp., Ridgewood, N.J., as well as Sisely and Wood, "Encyclopedia of Surface Active Agents", Chemical Publishing., Inc., New York, 1964, list surfactants and recommended uses. All formulations can contain minor amounts of additives to reduce foaming, caking, corrosion, microbiological growth, etc.

The methods of making such compositions are well known. Solutions are prepared by simply mixing the ingredients. Fine solid compositions are made by blending and, usually, grinding as in a hammer or fluid energy mill. Suspensions are prepared by wet milling (see, for example, Littler, U.S. Pat. No. 3,060,084). Granules and pellets may be made by spraying the active material upon preformed granular carriers or by agglomeration techniques. See J. E. Browning, "Agglomeration", Chemical Engineering, Dec. 4, 1967, pp. 147ff. and "Perry's Chemical Engineer's Handbook", 5th Ed., McGraw-Hill, New York, 1973, pp. 8-57ff.

For further information regarding the art of formulation, see for example:

H. M. Loux, U.S. Pat. No. 3,235,361, Feb. 15, 1966, Col. 6, line 16 through Col. 7, line 19 and Examples 10 through 41;

R. W. Luckenbaugh, U.S. Pat. No. 3,309,192, Mar. 14, 1967, Col. 5, line 43 through Col. 7, line 62 and Examples 8, 12, 15, 39, 41, 52, 53, 58, 132, 138-140, 162-164, 166, 167 and 169-182;

H. Gysin and E. Knusli, U.S. Pat. No. 2,891,855, June 23, 1959, Col. 3, line 66 through Col. 5, line 17 and Examples 1-4;

G. C. Klingman, "Weed Control as a Science", John Wiley and Sons, Inc., New York, 1961, pp. 81-96; and

J. D. Fryer and S. A. Evans, "Weed Control Handbook", 5th Ed., Blackwell Scientific Publications, Oxford, 1968, pp. 101-103.

In the following examples, all parts are by weight unless otherwise indicated.

EXAMPLE 8

    ______________________________________                                          Wettable Powder                                                               ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonl]-4-ethoxybenzoic                                 acid, methyl ester          80%                                                sodium alkylnaphthalenesulfonate                                                                           2%                                                 sodium ligninsulfonate      2%                                                 synthetic amorphous silica  3%                                                 kaolinite                   13%                                                ______________________________________                                    

The ingredients are blended, hammer-milled until all the solids are essentially under 50 microns, reblended, and packaged.

EXAMPLE 9

    ______________________________________                                          Wettable Powder                                                               ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester          50%                                                sodium alkylnaphthalenesulfonate                                                                           2%                                                 low viscosity methyl cellulose                                                                             2%                                                 diatomaceous earth          46%                                                ______________________________________                                    

The ingredients are blended, coarsely hammer-milled and then air-milled to produce particles essentially all below 10 microns in diameter. The product is reblended before packaging.

EXAMPLE 10

    ______________________________________                                          Granule                                                                       ______________________________________                                         Wettable Powder of Example 9                                                                          5%                                                      attapulgite granules   95%                                                     (U.S.S. 20-40 mesh; 0.84-0.42 mm)                                              ______________________________________                                    

A slurry of wettable powder containing 25% solids is sprayed on the surface of attapulgite granules while tumbling in a double-cone blender. The granules are dried and packaged.

EXAMPLE 11

    ______________________________________                                          Extruded Pellet                                                               ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester          25%                                                anhydrous sodium sulfate    10%                                                crude calcium ligninsulfonate                                                                              5%                                                 sodium alkylnaphthalenesulfonate                                                                           1%                                                 calcium/magnesium bentonite 59%                                                ______________________________________                                    

The ingredients are blended, hammer-milled and then moistened with about 12% water. The mixture is extruded as cylinders about 3 mm diameter which are cut to produce pellets about 3 mm long. These may be used directly after drying, or the dried pellets may be crushed to pass a U.S.S. No. 20 sieve (0.84 mm openings). The granules held on a U.S.S. No. 40 sieve (0.42 mm openings) may be packaged for use and the fines recycled.

EXAMPLE 12

    ______________________________________                                          Oil Suspension                                                                ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester          25%                                                polyoxyethylene sorbitol hexaoleate                                                                        5%                                                 highly aliphatic hydrocarbon oil                                                                           70%                                                ______________________________________                                    

The ingredients are ground together in a sand mill until the solid particles have been reduced to under about 5 microns. The resulting thick suspension may be applied directly, but preferably after being extended with oils or emulsified in water.

EXAMPLE 13

    ______________________________________                                          Wettable Powder                                                               ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester          20%                                                sodium alkylnaphthalenesulfonate                                                                           4%                                                 sodium ligninsulfonate      4%                                                 low viscosity methyl cellulose                                                                             3%                                                 attapulgite                 69%                                                ______________________________________                                    

The ingredients are thoroughly blended. After grinding in a hammer-mill to produce particles essentially all below 100 microns, the material is reblended and sifted through a U.S.S. No. 50 sieve (0.3 mm opening) and packaged.

EXAMPLE 14

    ______________________________________                                         Low Strength Granule                                                           ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester           l%                                                N,N--dimethylformamide       9%                                                attapulgite granules         90%                                               (U.S.S. 20-40 sieve)                                                           ______________________________________                                    

The active ingredient is dissolved in the solvent and the solution is sprayed upon dedusted granules in a double cone blender. After spraying of the solution has been completed, the blender is allowed to run for a short period and then the granules are packaged.

EXAMPLE 15

    ______________________________________                                         Aqueous Suspension                                                             ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester          40%                                                polyacrylic acid thickener  0.3%                                               dodecylphenol polyethylene glycol ether                                                                    0.5%                                               disodium phosphate          1%                                                 monosodium phosphate        0.5%                                               polyvinyl alcohol           1.0%                                               water                       56.7%                                              ______________________________________                                    

The ingredients are blended and ground together in a sand mill to produce particles essentially all under 5 microns in size.

EXAMPLE 16

    ______________________________________                                         Solution                                                                       ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester           5%                                                water                        95%                                               ______________________________________                                    

The salt is added directly to the water with stirring to produce the solution, which may then be packaged for use.

EXAMPLE 17

    ______________________________________                                         Low Strength Granule                                                           ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester          0.1%                                               attapulgite granules        99.9%                                              (U.S.S. 20-40 mesh)                                                            ______________________________________                                    

The active ingredient is dissolved in a solvent and the solution is sprayed upon dedusted granules in a double-cone blender. After spraying of the solution has been completed, the material is warmed to evaporate the solvent. The material is allowed to cool and then packaged.

EXAMPLE 18

    ______________________________________                                         Granule                                                                        ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester           80%                                               wetting agent                1%                                                crude ligninsulfonate salt (containing                                                                      10%                                               5-20% of the natural sugars)                                                   attapulgite clay             9%                                                ______________________________________                                    

The ingredients are blended and milled to pass through a 100 mesh screen. This material is then added to a fluid bed granulator, the air flow is adjusted to gently fluidize the material, and a fine spray of water is sprayed onto the fluidized material. The fluidization and spraying are continued until granules of the desired size range are made. The spraying is stopped, but fluidization is continued, optionally with heat, until the water content is reduced to the desired level, generally less than 1%. The material is then discharged, screened to the desired size range, generally 14-100 mesh (1410-149 microns), and packaged for use.

EXAMPLE 19

    ______________________________________                                         High Strength Concentrate                                                      ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester          99%                                                silica aerogel              0.5%                                               synthetic amorphous silica  0.5%                                               ______________________________________                                    

The ingredients are blended and ground in a hammer-mill to produce a material essentially all passing a U.S.S. No. 50 screen (0.3 mm opening). The concentrate may be formulated further if necessary.

EXAMPLE 20

    ______________________________________                                         Wettable Powder                                                                ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester          90%                                                dioctyl sodium sulfosuccinate                                                                              0.1%                                               synthetic fine silica       9.9%                                               ______________________________________                                    

The ingredients are blended and ground in a hammer-mill to produce particles essentially all below 100 microns. The material is sifted through a U.S.S. No. 50 screen and then packaged.

EXAMPLE 21

    ______________________________________                                         Wettable Powder                                                                ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester          40%                                                sodium ligninsulfonate      20%                                                montmorillonite clay        40%                                                ______________________________________                                    

The ingredients are thoroughly blended, coarsely hammer-milled and then air-milled to produce particles essentially all below 10 microns in size. The material is reblended and then packaged.

EXAMPLE 22

    ______________________________________                                         Oil Suspension                                                                 ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester          35%                                                blend of polyalcohol carboxylic                                                                            6%                                                 esters and oil soluble petroleum                                               sulfonates                                                                     xylene                      59%                                                ______________________________________                                    

The ingredients are combined and ground together in a sand mill to produce particles essentially all below 5 microns. The product can be used directly, extended with oils, or emulsified in water.

EXAMPLE 23

    ______________________________________                                         Dust                                                                           ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, ethyl ester           10%                                                attapulite                  10%                                                pyrophyllite                80%                                                ______________________________________                                    

The active ingredient is blended with attapulgite and then passed through a hammer-mill to produce particles substantially all below 200 microns. The ground concentrate is then blended with powdered pyrophyllite until homogeneous.

EXAMPLE 24

    ______________________________________                                         Emulsifiable Concentrate                                                       ______________________________________                                         2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-                                 yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic                                acid, methyl ester          20%                                                chlorobenzene               74%                                                sorbitan monostearate and polyoxyethylene                                      condensates thereof         6%                                                 ______________________________________                                    

The ingredients are combined and stirred to produce a solution which can be emulsified in water for application.

UTILITY

Test results indicate that the compounds of the present invention are highly active preemergent or postemergent herbicides or plant growth regulants. Many of them have utility for broad-spectrum pre- and/or postemergence weed control in areas where complete control of all vegetation is desired, such as around fuel storage tanks, ammunition depots, industrial storage areas, parking lots, drive-in theaters, around billboards, highway and railroad structures. Some of the compounds have utility for selective weed control in crops such as wheat, barley, corn and rice. Alternatively, the subject compounds are useful to modify plant growth.

The rates of application for the compounds of the invention are determined by a number of factors, including their use as plant growth modifiers or as herbicides, the crop species involved, the types of weeds to be controlled, weather and climate, formulations selected, mode of application, amount of foliage present, etc. In general terms, the subject compounds should be applied at levels of around 0.004 to 10 kg/ha, the lower rates being suggested for use on lighter soils and/or those having a low organic matter content, for plant growth modification or for situations where only short-term persistence is required.

The compounds of the invention may be used in combination with any other commercial herbicides. They are particularly useful in combination with the following herbicides.

    ______________________________________                                         Common Name Chemical Name                                                      ______________________________________                                         acifluorfen 5-[2-chloro-4-(trifluoromethyl)phenoxy]-                                       2-nitrobenzoic acid                                                acrolein    acrolein                                                           alachlor    2-chloro-2',6'-diethyl-N--(methoxymethyl)-                                     acetanilide                                                        ametryn     2-(ethylamino)-4-(isopropylamino)-6-                                           methylthio)- .sub.-s-triazine                                      amitrole    3-amino- .sub.-s-triazole                                          AMS         ammonium sulfamate                                                 asulam      methyl sulfanilylcarbamate                                         atrazine    2-chloro-4-(ethylamino)-6-(isopropyl-                                          amino)- .sub.-s-triazine                                           barban      4-chloro-2-butynyl  .sub.--m-chlorocarbanilate                     benefin     N--butyl-N--ethyl-α,α,α-trifluoro-2,6-                       dinitro- -p-toluidine                                              bensulide   O,O--diisopropyl phosphorodithioate                                            S--ester with N--(2-mercaptoethyl)-                                            benzenesulfonamide                                                 bentazon    3-isopropyl-1H--2,1,3-benzothiadiazin-                                         4(3H)--one 2,2-dioxide                                             benzipram   3,5-dimethyl-N--(1-methylethyl)-N--                                            (phenylmethyl)benzamide                                            benzoylprop N--benzoyl-N--(3,4-dichlorophenyl)-DL-                                         alaine                                                             bifenox     methyl 5-(2,4-dichlorophenoxy)-2-                                              nitrobenzoate                                                      bromacil    5-bromo-3-sec-butyl-6-methyluracil                                 bromoxynil  3,5-dibromo-4-hydroxybenzonitrile                                  butachlor   N--(butoxymethyl)-2-chloro-2',6'-                                              diethylacetanilide                                                 butam       2,2-dimethyl-N--(1-methylethyl)-N--                                            (phenylmethyl)propanamide                                          buthidazole 3-[5-(1,1-dimethylethyl)-1,3,4-thiadia-                                        zol-2-yl]-4-hydroxy-1-methyl-2-imida-                                          zolidinone                                                         butralin    4-(1,1-dimethylethyl)-N--(1-methyl-                                            propyl)-2,6-dinitrobenzenamine                                     butylate    S--ethyl-diisobutylthiocarbamate                                   cacodylic   hydroxydimethylarsine oxide                                        acid                                                                           carbetamide D-N--ethyllactamide carbanilate (ester)                            CDAA        N--N--diallyl-2-chloroacetamide                                    CDEC        2-chloroallyl diethyldithiocarbamate                               chlorbromuron                                                                              3-(4-bromo-3-chlorophenyl)-1-methoxy-1-                                        methylurea                                                         chloroxuron 3-[ -p-( -p-chlorophenoxy)phenyl]  -1,1-                                       dimethylurea                                                       chlorpropham                                                                               isopropyl  .sub.--m-chlorocarbanilate                              chlorsulfuron                                                                              2-chloro-N--[(4-methoxy-6-methyl-1,3,5-                                        triazin-2-yl)aminocarbonyl]benzene-                                            sulfonamide                                                        chlortoluron                                                                               N'--(3-chloro-4-methylphenyl-N',N'--                                           dimethylurea                                                       cisanilide  cis-2,5-dimethyl-N--phenyl-1-pyrrolidine-                                      carboxamide                                                        CMA         calcium methanearsonate                                            cyanazine   2-[[4-chloro-6-(ethylamino)- .sub.-s-triazin-2-                                yl]amino]-2-methylpropionitrile                                    cycloate    S--ethyl N--ethylthiocyclohexanecarbamate                          cycluron    3-cyclooctyl-1,1-dimethylurea                                      cyperquat   1-methyl-4-phenylpyridinium                                        cyprazine   2-chloro-4-(cyclopropylamino)-6-(iso-                                          propylamino)- .sub.-s-triazine                                     cyprazole   N--[5-(2-chloro-1,1-dimethylethyl)-1,3,4-                                      thiadiazol-2-yl] cyclopropanecarbox-                                           amide                                                              cypromid    3',4'-dichlorocyclopropanecarboxanilide                            dalapon     2,2-dichloropropionic acid                                         dazomet     tetrahydro-3,5-dimethyl-2H--1,3,5-thia-                                        diazine-2-thione                                                   DCPA        dimethyl tetrachloroterephthalate                                  desmetryn   2-(isopropylamino)-4-(methylamino)-6-                                          methylthio)- .sub.-s-triazine                                      diallate    S--(2,3-dichloroallyl)diisopropylthio-                                         carbamate                                                          dicamba     3,6-dichloro- -o-anisic acid                                       dichlobenil 2,6-dichlorobenzonitrile                                           dichlorprop 2-(2,4-dichlorophenoxy)propionic acid                              diclofop    2-[4-(2,4-dichlorophenoxy)phenoxy]-                                            propanoic acid                                                     diethatyl   N--(chloroacetyl)-N--(2,6-diethylphenyl)-                                      glycine                                                            difenzoquat 1,2-dimethyl-3,5-diphenyl-1H--pyrazolium                           dinitramine N.sup.4,N.sup.4 --diethyl-α,α,α-trifluoro-3,                 5-                                                                             dinitrotoluene-2,4-diamine                                         dinoseb     2-sec-butyl-4,6-dinitrophenol                                      diphenamide N,N--dimethyl-2,2-diphenylacetamide                                dipropetryn 2-(ethylthio)-4,6-bis(isopropylamino)-                                         s-triazine                                                         diquat      6,7-dihydrodipyrido[1,2-α:2',1'-c]-                                      pyrazinediium ion                                                  diuron      3-(3,4-dichlorophenyl)-1,1-dimethylurea                            DSMA        disodium methanearsonate                                           endothall   7-oxabicyclo[2.2.1]heptane-2,3-dicarbox-                                       ylic acid                                                          erbon       2-(2,4,5-trichlorophenoxy)ethyl 2,2-                                           dichloropropionate                                                 ethafluralin                                                                               N--ethyl-N--(2-methyl-2-propenyl)-2,6-                                         dinitro-4-(trifluoromethyl)benzen-                                             amine                                                              ethofumesate                                                                               (±)-2-ethoxy-2,3-dihydro-3,3-dimethyl-                                      5-benzofuranyl methanesulfonate                                    fenac       (2,3,6-trichlorophenyl)acetic acid                                 fenoxaprop  ethyl 2-(4-(6-chloro-2-benzoxazolyl-                               ethyl       oxy)phenoxy)propanoate                                             fenuron     1,1-dimethyl-3-phenylurea                                          fenuron TCA 1,1-dimethyl-3-phenylurea mono(tri-                                            chloroacetate)                                                     flamprop    N--benzoyl-N--(3-chloro-4-fluorophenyl)-                                       DL-alanine                                                         fluchloralin                                                                               N--(2-chloroethyl)-2,6-dinitro-N--propyl-                                      4-(trifluoromethyl)aniline                                         fluometuron 1,1-dimethyl-3-(α,α,α-trifluoro- .sub.--m-to                 lyl)-                                                                          urea                                                               fluorodifen  -p-nitrophenyl α,α,α-trifluoro-2-nitro-                      -p-tolyl ether                                                    fluridone   1-methyl-3-phenyl-5-[3-(trifluoro-                                             methyl)phenyl]-4(1H)--pyridinone                                   fomesafen   5-(2-chloro-4-trifluoromethylphenoxy)-                                         N--methylsulfonyl-2-nitrobenzamide                                 fosamine    ethyl hydrogen (aminocarbonyl)phos-                                            phonate                                                            glyphosate  N--(phosphonomethyl)glycine                                        hexaflurate potassium hexafluoroarsenate                                       hexazinone  3-cyclohexyl-6-(dimethylamino)-1-methyl-                                       1,3,5-triazine-2,4(1H,3H)--dione                                   imazaquin   2-(4,5-dihydro-4-methyl-4-(1-methyl-                                           ethyl)-5-oxo-1H--imidazol-2-yl)-3-                                             quinolinecarboxylic acid                                           ioxynil     4-hydroxy-3,5-diiodobenzonitrile                                   isopropalin 2,6-dinitro-N,N--dipropylcumidine                                  karbutilate tert-butylcarbamic acid ester with 3-( .sub.--m-                               hydroxyphenyl)-1,1-dimethylurea                                    lactofen    1'-(carboethoxy)ethyl-5-(2-chloro-4-                                           (trifluoromethyl)phenoxy)-2-nitro-                                             benzoate                                                           lenacil     3-cyclohexyl-6,7-dihydro-1H--cyclopenta-                                       pyrimidine-2,4(3H,5H)--dione                                       linuron     3-(3,4-dichlorophenyl)-1-methoxy-1-                                            methylurea                                                         MAA         methanearsonic acid                                                MAMA        monoammonium methanearsonate                                       MCPA        [(4-chloro- -o-tolyl)oxy]acetic acid                               MCPB        4-[(4-chloro- -o-tolyl)oxy]butyric acid                            mecoprop    2-[(4-chloro- -o-tolyl)oxy]propionic acid                          mefluidide  N--[(2,4-dimethyl-5-[[(trifluoromethyl)-                                       sulfonyl]amino]phenyl]acetamide                                    methal-     N--(2-methyl-2-propenyl)-2,6-dinitro-N--                           propalin    propyl-4-(trifluoromethyl)benzenamide                              methabenz-  1,3-dimethyl-3-(2-benzothiazolyl)urea                              thiazuron                                                                      metham      sodium methyldithiocarbamate                                       methazole   2-(3,4-dichlorophenyl)-4-methyl-1,2,4-                                         oxadiazolidine-3,5-dione                                           methoxuron  N'--(3-chloro-4-methoxyphenyl)N,N--                                            dimethylurea                                                       metolachlor 2-chloro-N--(2-ethyl-6-methylphenyl)-N--                                       (2-methoxy-1-methylethyl)acetamide                                 metribuzin  4-amino-6-tert-butyl-3-(methylthio)-as-                                        triazine-5(4H)--one                                                metsulfuron 2-[[(4-methoxy-6-methyl-1,3,5-triazine-                            methyl      2-yl)aminocarbonyl]aminosulfonyl]ben-                                          zoic acid, methyl ester                                            molinate    S--ethyl hexahydro-1H--azepine-1-carbo-                                        thioate                                                            monolinuron 3-( -p-chlorophenyl)-1-methoxy-1-methyl-                                       urea                                                               monuron     3-( -p-chlorophenyl)-1,1-dimethylurea                              monuron TCA 3-( -p-chlorophenyl)-1,1-dimethylurea                                          mono(trichloroacetate)                                             MSMA        monosodium methanearsonate                                         napropamide 2-(α-naphthoxy)-N,N--diethylpropion-                                     amide                                                              naptalam    N--1-naphthylphthalamic acid                                       neburon     1-butyl-3-(3,4-dichlorophenyl)-1-methyl-                                       urea                                                               nitralin    4-(methylsulfonyl)-2,6-dinitro-N,N--                                           dipropylaniline                                                    nitrofen    2,4-dichlorophenyl  -p-nitrophenyl ether                           nitrofluorfen                                                                              2-chloro-1-(4-nitrophenoxy)-4-(tri-                                            fluoromethyl)benzene                                               norea       3-(hexahydro-4,7-methanoindan-5-yl)-1,1-                                       dimethylurea                                                       norflurazon 4-chloro-5-(methylamino)-2-(α,α,α-tri-                       fluoro- .sub.--m-tolyl)-3(2H)--pyridazinone                        oryzalin    3,4-dinitro-N,N--dipropylsulfanilamide                             oxadiazon   2-tert-butyl-4-(2,4-dichloro-5-isopro-                                         poxyphenyl)Δ.sup.2 -1,3,4-oxadiazolin-5-one                  oxyfluorfen 2-chloro-1-(3-ethoxy-4-nitrophenoxy)-4-                                        (trifluoromethyl)benzene                                           paraquat    1,1'-dimethyl-4,4'-bipyridinium ion                                PBA         chlorinated benzoic acid                                           pendimethalin                                                                              N--(1-ethylpropyl)-3,4-dimethyl-2,6-                                           dinitrobenzenamine                                                 perfluidone 1,1,1-trifluoro-N--[2-methyl-4-(phenyl-                                        sulfonyl)phenyl]methanesulfonamide                                 picloram    4-amino-3,5,6-trichloropicolinic acid                              procyazine  2-[[4-chloro-6-(cyclopropylamino)-1,3,5-                                       triazine-2-yl]amino]-2-methylpropane-                                          nitrile                                                            profluralin N--(cyclopropylmethyl)-α,α,α-trifluoro-                      2,6-dinitro-N--propyl- -p-toluidine                                prometon    2,4-bis(isopropylamino)-6-methoxy- .sub.-s-                                    triazine                                                           prometryn   2,4-bis(isopropylamino)-6-(methylthio)-                                         .sub.-s-triazine                                                  pronamide   3,5-dichloro N--(1,1-dimethyl-2-propyn-                                        yl)benzamide                                                       propachlor  2-chloro-N--isopropylacetanilide                                   propanil    3',4'-dichloropropionalide                                         propazine   2-chloro-4,6-bis(isopropylamino)- .sub.-s-                                     triazine                                                           propham     isopropyl carbanilate                                              prosulfalin N--[[4-(dipropylamino)-3,5-dinitro-                                            phenyl]sulfonyl]-S,S--dimethylsulfil-                                          imine                                                              prynachlor  2-chloro-N--(1-methyl-2-propynyl)acet-                                         anilide                                                            quinofop    2-[4-(6-chloroquinoxalin-2-yloxy)phen-                             ethyl       oxypropanoic acid, ethyl ester                                     secbumeton  N--ethyl-6-methoxy-N'(1-methylpropyl)-                                         1,3,5-triazine-2,4-diamine                                         sethoxydim  2-[1-(ethoxyimino)butyl]-5-[2-(ethyl-                                          thio)propyl]-3-hydroxy-2-cyclohexene-                                          1-one                                                              siduron     1-(2-methylcyclohexyl)-3-phenylurea                                simazine    2-chloro-4,6-bis(ethylamino)- .sub.-s-triazine                     simetryn    2,4-bis(ethylamino)-6-(methylthio)- .sub.-s-                                   triazine                                                           supriox     2-[1-(2,5-dimethylphenyl)ethylsulfonyl]  -                                     pyridine-N--oxide                                                  TCA         trichloroacetic acid                                               tebuthiuron N--[5-(1,1-dimethylethyl)-1,3,4-thiadi-                                        azol-2-yl]-N,N'--dimethylurea                                      terbacil    3-tert-butyl-5-chloro-6-methyluracil                               terbuchlor  N--(butoxymethyl)-2-chloro-N--[2-(1,1-                                         dimethylethyl)-6-methylphenyl]-                                                acetamide                                                          terbuthyl-  2-(tert-butylamino)-4-chloro-6-(ethyl-                             azine       amino)- .sub.-s-triazine                                           terbutol    2,6-di-tert-butyl- -p-tolyl methylcar-                                         bamate                                                             terbutryn   2-(tert-butylamino)-4-(ethylamino)-6-                                          (methylthio)- .sub.-s-triazine                                     tetrafluron N,N--dimethyl-N'--[3-(1,1,2,2-tetrafluoro-                                     ethoxy)phenyl]urea                                                 thiobencarb S--[(4-chlorophenyl)methyl] diethylcar-                                        bamothioate                                                        triallate   S--(2,3,3-trichloroallyl)diisopropylthio-                                      carbamate                                                          trifluralin α,α,α-trifluoro-2,6-dinitro-N,N--propyl-                      -p-toluidine                                                      trimeturon  1-( -p-chlorophenyl)-2,3,3-trimethylpseu-                                      dourea                                                             vernolate   S--propyl dipropylthiocarbamate                                                ethyl 5-[2-chloro-4-(trifluoromethyl)-                                         phenoxy]-2-nitrobenzoic acid                                       2,3,6-TBA.sup.b                                                                            2,3,6-trichlorobenzoic acid                                        2,4-D       (2,4-dichlorophenoxy)acetic acid                                   2,4-DB      4-(2,4-dichlorophenoxy)butyric acid                                2,4-DEP     tris[2-(2,4-dichlorophenoxy)ethyl]                                             phosphite                                                          ______________________________________                                         Trade Name or                                                                  Code Number Chemical Name                                                      ______________________________________                                         "Cinch"     exo-1-methyl-4-(1-methylethyl)-2-[(2-                                          methylphenyl)methoxy]-7-oxabicyclo-                                            [2.2.1]heptane                                                     AC 263,499  2-[4,5-dihydro-4-methyl-4-(1-methyl-                                           ethyl)-5-oxo-1H--imidazol-2-yl]-5-                                             ethyl-3-pyridinecarboxylic acid                                    Harmony ™                                                                               3-[[(4-methoxy-6-methyl-1,3,5-triazin-                                         2-yl)aminocarbonyl]aminosulfonyl]-2-                                           thiophenecarboxylic acid, methyl ester                             PPG-1013    5-(2-chloro-4-(trifluoromethyl)phenoxy)-                                       2-nitroacetophenone oxime-O--acetic                                            acid, methyl ester                                                 DOWCO 453 ME                                                                               2-(4-(3-chloro-5-trifluoromethylpyridin-                                       2-yloxy)phenoxy)propanoic acid, methyl                                         ester                                                              FMC 57020   2-(2'-chlorophenyl)methyl-4,4-dimethyl-                                        3-isoxazolidinone                                                  AC 222,293  6-(4-isopropyl-4-methyl-5-oxo-2-imid-                                          azolin-2-yl)- .sub.--m-toluic acid, methyl                                     ester and 6-(4-isopropyl-4-methyl-5-                                           oxo-2-imidazolin-2-yl- -p-toluic acid,                                         methyl ester                                                       AC 252,925  2-(4-isopropyl-4-methyl-5-oxo-2-imidazo-                                       lin-2-yl)nicotinic acid with isopropyl                                         amine (1:1)                                                        DPX-L5300   2-[[N--(4-methoxy-6-methyl-1,3,5-tria-                                         zine-2-yl)-N--methylaminocarbonyl]-                                            aminosulfonyl]benzoic acid, methyl                                             ester                                                              --          2-Butyl-2,3-dihydro-N--[(4-methoxy-6-                                          methylpyrimidin-2-yl)aminocarbonyl]-                                           1,2-benzisothiazole-7-sulfonamide-                                             1,1-dioxide                                                        --          2-Butyl-2,3-dihydro-N--[(4,6-dimethoxy-                                        pyrimidin-2-yl)aminocarbonyl]-1,2-                                             benzisothiazole-7-sulfonamide-1,1-                                             dioxide                                                            ______________________________________                                    

The herbicidal properties of the subject compounds were discovered in a number of greenhouse tests. The test procedures and results follow.

TEST A

Seeds of crabgrass (Digitaria sp.), barnyardgrass (Echinochloa crusgalli), wild oats (Avena fatua), sicklepod (Cassia obtusifolia), morningglory (Ipomoea spp.), cocklebur (Xanthium pensylvanicum), sorghum, corn, soybean, sugar beet, cotton, rice, wheat and purple nutsedge (Cyperus rotundus) tubers were planted and treated preemergence with the test chemicals dissolved in a non-phytotoxic solvent. At the same time, these crop and weed species were treated with a soil/foliage application. At the time of treatment, the plants ranged in height from 2 to 18 cm. Treated plants and controls were maintained in a greenhouse for sixteen days, after which all species were compared to controls and visually rated for response to treatment. The ratings, summarized in Table A, are based on a numerical scale extending from 0=no injury, to 10=complete kill. The accompanying descriptive symbols have the following meanings:

B=burn;

C=chlorosis/necrosis;

D=defoliation;

E=emergence inhibition;

G=growth retardation;

H=formative effects;

S=albinism;

U=unusual pigmentation;

X=axillary stimulation; and

6Y=abscised buds or flowers.

--=no test

    ______________________________________                                         Compounds                                                                       ##STR37##                                                                     Compound   R.sub.1    R.sub.2     Y                                            ______________________________________                                         1          CH.sub.3   OCH.sub.3   OCH.sub.3                                    2          CH.sub.3 CH.sub.2                                                                         OCH.sub.3   OCH.sub.3                                    3          CH.sub.3 CH.sub.2                                                                         OCH.sub.3   OCF.sub.2 H                                  4          CH.sub.3 CH.sub.2                                                                         OCH.sub.3   CH.sub.3                                     5          CH.sub.3   OCH.sub.2 CH.sub.3                                                                         OCH.sub.3                                    6          CH.sub.3   SCH.sub.3   OCH.sub.3                                    ______________________________________                                    

                  TABLE A                                                          ______________________________________                                                       Cmpd. 1    Cmpd. 2  Cmpd. 3                                      Rate kg/ha    0.05       0.05     0.05                                         ______________________________________                                         POSTEMERGENCE                                                                  Morningglory  9C         10C      9C                                           Cocklebur     10C        3C,8H    5C,9G                                        Nutsedge      9C         9G       9G                                           Crabgrass     3C,6G      0        4G                                           Barnyardgrass 5C,9H      3C,3H    1C                                           Wild Oats     2G         0        0                                            Wheat         2G         0        0                                            Corn          3C,9H      0        1C                                           Soybean       5C,9G      3C,8G    3C,8H                                        Rice          3C,6G      0        0                                            Sorghum       3C,9H      9H       3C,9H                                        Sugar beet    10C        10C      9C                                           Cotton        9C         9G       9G                                           SicklePod     9C         9C       4C,5H                                        PREEMERGENCE                                                                   Morningglory  9G         8G       9G                                           Cocklebur     8H         8G       3C,5H                                        Nutsedge      10E        10E      10E                                          Crabgrass     0          0        2G                                           Barnyardgrass 5C,9H      6G       4G                                           Wild Oats     2C,3H      2C       1C                                           Wheat         6G         2C,4G    0                                            Corn          2C,8G      5G       5G                                           Soybean       3C,8H      2C,7H    1H                                           Rice          8G         5G       2G                                           Sorghum       6C,9H      3C,9H    3C,9H                                        Sugar beet    5C,9G      10E      3C,8G                                        Cotton        9G         6G       7G                                           Sicklepod     2C,7G      2C,4G    2G                                                         Cmpd. 4    Cmpd. 5  Cmpd. 6                                      ______________________________________                                         Rate kg/ha    0.05       0.05     0.05                                         ______________________________________                                         POSTEMERGENCE                                                                  Morningglory  2C,2H      10C      10C                                          Cocklebur     3C,8G      10C      5C,9G                                        Nutsedge      5G         4C,8G    2C,9G                                        Crabgrass     3G         2G       1H                                           Barnyardgrass 1C         3H       4C,9H                                        Wild Oats     1C         0        4C,8G                                        Wheat         2G         0        5C,9G                                        Corn          0          1H       4C,9H                                        Soybean       2C,2H      5C,9G    5C,9G                                        Rice          1C         5G       4C,8G                                        Sorghum       2C,6G      2C,5G    9C                                           Sugar beet    3C,5G      10C      9C                                           Cotton        2C,8G      9C       9C                                           Sicklepod     3C,5G      9C       9C                                           PREEMERGENCE                                                                   Morningglory  9C         9G       9G                                           Cocklebur     --         8H       9H                                           Nutsedge      10E        3C,7G    10E                                          Crabgrass     0          0        2C                                           Barnyardgrass 5G         3C       5C,9H                                        Wild Oats     5G         2C       5C,9G                                        Wheat         5G         4C       10C                                          Corn          5G         2C,7G    9G                                           Soybean       0          8H       4C,7H                                        Rice          2C,7G      2C,8G    9H                                           Sorghum       2C,5G      7G       9H                                           Sugar beet    2G         9C       5C,9G                                        Cotton        7G         8G       8G                                           Sicklepod     9G         3C       3C,7G                                        ______________________________________                                    

TEST B Postemergence

Two round pans (25 cm diameter by 12.5 cm deep) were filled with Sassafras sandy loam soil. One pan was planted with blackgrass (Alopecurus myosuroides), sugar beets, nutsedge (Cyperus rotundus) tubers, rape (Brassica napus), crabgrass (Digitaria sanguinalis), sicklepod (Cassia obtusifolia), teaweed (Sida spinosa), jimsonweed (Datura stramonium), velvetleaf (Abutilon theophrasti), and giant foxtail (Setaria faberii). The other pan was planted with wheat, cotton, rice, corn, soybean, wild oats (Avena fatua), cocklebur (Xanthium pensylvanicum), morningglory (Ipomoea hederacea), johnsongrass (Sorghum halepense) and barnyardgrass (Echinochloa crusgalli). The plants were grown for approximately fourteen days, then sprayed postemergence with the chemicals dissolved in a non-phytotoxic solvent.

Preemergence

Two round pans (25 cm diameter by 12.5 cm deep) were filled with Sassafras sandy loam soil. One pan was planted with blackgrass, sugar beets, nutsedge, rape, crabgrass, sicklepod, teaweed, jimsonweed, velvetleaf, and giant foxtail. The other pan was planted with wheat, cotton, rice, corn, soybeans, wild oats, cocklebur, morningglory, johnsongrass, and barnyardgrass. The two pans were sprayed preemergence with the chemicals dissolved in a non-phytotoxic solvent.

Treated plants and controls were maintained in the greenhouse for 28 days, then all treated plants were compared to controls and visually rated for plant response.

Response ratings are based on a scale of 0 to 100 where 0=no effect, and 100=complete control. A dash (--) response means no test.

Response ratings are contained in Table B.

                  TABLE B                                                          ______________________________________                                         Compound 1                                                                     POSTEMERGENCE                                                                  Rate g/ha       62     16      4      1                                        ______________________________________                                         Corn            100    90      80     40                                       Wheat           0      0       0      0                                        Rice            100    100     60     50                                       Soybean         100    100     100    80                                       Cotton          100    100     90     30                                       Sugar beet      100    100     100    90                                       Rape            100    100     100    80                                       Crabgrass       50     30      0      0                                        Johnsongrass    40     30      0      0                                        Blackgrass      100    100     90     60                                       Barnyardgrass   50     0       0      0                                        Nutsedge        100    100     90     40                                       Giant Foxtail   20     0       0      0                                        Wild Oats       30     0       0      0                                        Cocklebur       100    100     90     50                                       Morningglory    100    100     90     80                                       Teaweed         90     50      0      0                                        Sicklepod       100    100     70     20                                       Jimsonweed      100    90      40     0                                        Velvetleaf      100    100     100    80                                       ______________________________________                                         PREEMERGENCE                                                                   Rate g/ha         250    62       16                                           ______________________________________                                         Corn              100    60       20                                           Wheat             0      0        0                                            Rice              100    100      80                                           Soybean           90     20       0                                            Cotton            80     30       0                                            Sugar beet        100    90       70                                           Rape              100    90       70                                           Crabgrass         70     50       0                                            Johnsongrass      90     90       30                                           Blackgrass        100    100      80                                           Barnyardgrass     90     60       0                                            Nutsedge          100    90       50                                           Giant Foxtail     60     20       0                                            Wild Oats         70     40       0                                            Cocklebur         90     80       60                                           Morningglory      90     90       60                                           Teaweed           90     80       20                                           Sicklepod         90     80       30                                           Jimsonweed        100    90       80                                           Velvetleaf        100    100      90                                           ______________________________________                                         Compound 2                                                                     POSTEMERGENCE                                                                  Rate g/ha       250    62      16     4                                        ______________________________________                                         Corn            70     30      0      0                                        Wheat           40     0       0      0                                        Rice            50     0       0      0                                        Soybean         100    100     100    80                                       Cotton          70     40      20     0                                        Sugar beet      100    100     90     80                                       Rape            100    100     100    80                                       Crabgrass       30     0       0      0                                        Johnsongrass    100    70      30     0                                        Blackgrass      100    100     60     20                                       Barnyardgrass   70     50      20     0                                        Nutsedge        100    100     90     40                                       Giant Foxtail   60     20      0      0                                        Wild Oats       20     0       0      0                                        Cocklebur       100    100     100    80                                       Morningglory    100    100     90     50                                       Teaweed         80     40      20     0                                        Sicklepod       100    100     80     20                                       Jimsonweed      100    70      30     0                                        Velvetleaf      100    100     100    60                                       ______________________________________                                         PREEMERGENCE                                                                   Rate g/ha       250    62      16     4                                        ______________________________________                                         Corn            60     30      0      0                                        Wheat           0      0       0      0                                        Rice            90     80      70     30                                       Soybean         90     60      20     0                                        Cotton          20     0       0      0                                        Sugar beet      100    100     70     30                                       Rape            100    100     90     50                                       Crabgrass       50     0       0      0                                        Johnsongrass    100    70      0      0                                        Blackgrass      100    100     100    80                                       Barnyardgrass   60     50      0      0                                        Nutsedge        100    80      30     0                                        Giant Foxtail   60     20      0      0                                        Wild Oats       0      0       0      0                                        Cocklebur       80     60      40     30                                       Morningglory    80     70      40     0                                        Teaweed         80     80      30     0                                        Sicklepod       80     40      0      0                                        Jimsonweed      100    100     30     0                                        Velvetleaf      100    100     40     0                                        ______________________________________                                         Compound 3                                                                     POSTEMERGENCE                                                                  Rate g/ha         250    62       16                                           ______________________________________                                         Corn              0      0        0                                            Wheat             0      0        0                                            Rice              0      0        0                                            Soybean           90     80       20                                           Cotton            60     0        0                                            Sugar beet        30     0        0                                            Rape              100    90       60                                           Crabgrass         0      0        0                                            Johnsongrass      90     50       20                                           Blackgrass        100    90       80                                           Barnyardgrass     50     20       0                                            Nutsedge          80     50       0                                            Giant Foxtail     30     0        0                                            Wild Oats         0      0        0                                            Cocklebur         90     80       50                                           Morningglory      0      0        0                                            Teaweed           60     20       0                                            Sicklepod         60     0        0                                            Jimsonweed        90     70       20                                           Velvetleaf        100    70       30                                           ______________________________________                                         PREEMERGENCE                                                                   Rate g/ha         250    62       16                                           ______________________________________                                         Corn              20     0        0                                            Wheat             20     0        0                                            Rice              90     90       20                                           Soybean           20     0        0                                            Cotton            0      0        0                                            Sugar beet        90     70       20                                           Rape              100    90       50                                           Crabgrass         60     0        0                                            Johnsongrass      l00    90       40                                           Blackgrass        100    90       80                                           Barnyardgrass     80     60       20                                           Nutsedge          90     80       60                                           Giant Foxtail     70     40       0                                            Wild Oats         0      0        0                                            Cocklebur         90     50       0                                            Morningglory      60     0        0                                            Teaweed           80     30       0                                            Sicklepod         0      0        0                                            Jimsonweed        90     70       20                                           Velvetleaf        90     60       0                                            ______________________________________                                         Compound 4                                                                     POSTEMERGENCE                                                                  Rate g/ha         250    62       16                                           ______________________________________                                         Corn              10     0        0                                            Wheat             70     20       0                                            Rice              0      0        0                                            Soybean           10     0        0                                            Cotton            70     40       0                                            Sugar beet        20     0        0                                            Rape              70     50       0                                            Crabgrass         0      0        0                                            Johnsongrass      90     70       30                                           Blackgrass        80     70       0                                            Barnyardgrass     80     50       0                                            Nutsedge          30     0        0                                            Giant Foxtail     30     0        0                                            Wild Oats         0      0        0                                            Cocklebur         90     80       50                                           Morningglory      0      0        0                                            Teaweed           50     0        0                                            Sicklepod         30     0        0                                            Jimsonweed        70     60       0                                            Velvetleaf        80     70       20                                           ______________________________________                                         PREEMERGENCE                                                                   Rate g/ha         250    62       16                                           ______________________________________                                         Corn              0      0        0                                            Wheat             0      0        0                                            Rice              80     30       0                                            Soybean           0      0        0                                            Cotton            20     0        0                                            Sugar beet        0      0        0                                            Rape              90     60       20                                           Crabgrass         70     30       0                                            Johnsongrass      80     50       0                                            Blackgrass        90     70       40                                           Barnyardgrass     70     40       0                                            Nutsedge          90     70       20                                           Giant Foxtail     60     40       0                                            Wild Oats         30     0        0                                            Cocklebur         50     0        0                                            Morningglory      0      0        0                                            Teaweed           80     60       30                                           Sicklepod         30     0        0                                            Jimsonweed        90     70       20                                           Velvetleaf        80     30       0                                            ______________________________________                                         Compound 5                                                                     POSTEMERGENCE                                                                  Rate g/ha       62     16      4      1                                        ______________________________________                                         Corn            0      0       0      0                                        Wheat           0      0       0      0                                        Rice            0      0       0      0                                        Soybean         100    100     90     30                                       Cotton          50     30      20     0                                        Sugar beet      100    100     90     40                                       Rape            100    100     100    60                                       Crabgrass       30     0       0      0                                        Johnsongrass    40     20      0      0                                        Blackgrass      90     70      20     0                                        Barnyardgrass   0      0       0      0                                        Nutsedge        0      0       0      0                                        Giant Foxtail   0      0       0      0                                        Wild Oats       0      0       0      0                                        Cocklebur       100    80      30     0                                        Morningglory    100    100     30     0                                        Teaweed         30     0       0      0                                        Sicklepod       30     0       0      0                                        Jimsonweed      80     50      20     0                                        Velvetleaf      100    100     40     0                                        ______________________________________                                         PREEMERGENCE                                                                   Rate g/ha         250    62       16                                           ______________________________________                                         Corn              20     0        0                                            Wheat             0      0        0                                            Rice              100    80       0                                            Soybean           40     0        0                                            Cotton            0      0        0                                            Sugar beet        100    60       0                                            Rape              100    90       30                                           Crabgrass         0      0        0                                            Johnsongrass      30     0        0                                            Blackgrass        100    90       90                                           Barnyardgrass     50     0        0                                            Nutsedge          50     0        0                                            Giant Foxtail     20     0        0                                            Wild Oats         0      0        0                                            Cocklebur         90     90       70                                           Morningglory      80     30       0                                            Teaweed           80     70       30                                           Sicklepod         70     30       0                                            Jimsonweed        90     80       70                                           Velvetleaf        90     80       50                                           ______________________________________                                         Compound 6                                                                     POSTEMERGENCE                                                                  Rate g/ha         62     16       4                                            ______________________________________                                         Corn              80     40       20                                           Wheat             50     0        0                                            Rice              70     0        0                                            Soybean           100    90       80                                           Cotton            70     70       0                                            Sugarbeet         100    90       70                                           Rape              100    90       80                                           Crabgrass         40     0        0                                            Johnsongrass      100    90       50                                           Blackgrass        100    90       80                                           Barnyardgrass     70     30       0                                            Nutsedge          100    70       0                                            Giant Foxtail     50     20       0                                            Wild Oats         50     0        0                                            Cocklebur         100    90       70                                           Morningglory      l00    l00      70                                           Teaweed           80     20       0                                            Sicklepod         90     20       0                                            Jimsonweed        90     90       60                                           Velvetleaf        100    90       20                                           ______________________________________                                         PREEMERGENCE                                                                   Rate g/ha        250    62      16    4                                        ______________________________________                                         Corn             90     30      0     0                                        Wheat            90     20      0     0                                        Rice             100    100     80    60                                       Soybean          90     60      20    0                                        Cotton           40     0       0     0                                        Sugar beet       100    90      80    40                                       Rape             100    90      80    20                                       Crabgrass        50     0       0     0                                        Johnsongrass     90     90      30    0                                        Blackgrass       100    100     90    70                                       Barnyardgrass    100    90      30    0                                        Nutsedge         100    80      0     0                                        Giant Foxtail    100    90      40    0                                        Wild Oats        90     80      60    60                                       Cocklebur        90     80      50    0                                        Morningglory     90     80      30    0                                        Teaweed          80     60      20    0                                        Sicklepod        80     70      0     0                                        Jimsonweed       90     90      60    20                                       Velvetleaf       100    80      60    0                                        ______________________________________                                    

TEST C

Two ten-inch in diameter plastic pans lined with polyethylene liners were filled with prepared Fallsington silt loam soil. One pan was planted with seeds of wheat (Triticum aestivum), barley (Hordeum vulgare), wild oats (Avena fatua), cheatgrass (Bromus secalinus), blackgrass (Alopecurus myosuroides), annual bluegrass (Poa annua), green foxtail (Setaria viridis), rapeseed (Brassica napus) and Italian ryegrass (Lolium multiflorum). The other pan was planted with seeds of Russian thistle (Salsola kali), kochia (Kochia scoparia), speedwell (Veronica persica), shepherd's purse (Capsella bursa-pastoris), Matricaria inodora, black nightshade (Solanum nigrum), wild buckwheat (Polygonum convolvulus), Galium aparine and sugar beets. The above two pans were treated preemergence. At the same time two pans in which the above plant species were growing were treated postemergence. Plant height at the time of treatment ranged from 1-15 cm depending on plant species.

The compounds applied were diluted with a nonphytotoxic solvent and sprayed over-the-top of the pans. An untreated control and a solvent alone control were included for comparison. All treatments were maintained in the greenhouse for 20 days at which time the treatments were compared to the controls and the effects visually rated. The recorded data are presented in Table C.

                  TABLE C                                                          ______________________________________                                                       Compound 3                                                                     Postemergence                                                    Rate kg/ha      0.125  0.064     0.032                                                                               0.016                                    ______________________________________                                         wheat           0      0         0    0                                        barley          0      2G        0    0                                        wild oats       0      0         0    0                                        cheatgrass      0      0         0    0                                        blackgrass      9G     8G        7G   6G                                       annual bluegrass                                                                               3G     0         0    0                                        green foxtail   0      0         0    0                                        Italian ryegrass                                                                               2G     0         0    0                                        rapeseed        8G     7G        5G   3G                                       Matricaria inodora                                                                             10C    8G        5G   4G                                       galium aparine  8G     10C       3G   5G                                       Russian thistle 0      0         0    0                                        shepherd's purse                                                                               10C    10C       10C  10C                                      kochia          0      0         0    0                                        black nightshade                                                                               0      0         0    0                                        speedwell       5G     3G        0    0                                        wild buckwheat  0      0         0    0                                        sugar beet      4G     5G        4G   2G                                       ______________________________________                                                       Postemergence                                                    Rate kg/ha      0.008  0.004     0.002                                         ______________________________________                                         wheat           0      0         0                                             barley          0      0         0                                             wild oats       0      0         0                                             cheatgrass      0      0         0                                             blackgrass      6G     2G        0                                             annual bluegrass                                                                               0      0         0                                             green foxtail   0      0         0                                             Italian ryegrass                                                                               0      0         0                                             rapeseed        3G     2G        0                                             Matricaria inodora                                                                             4G     4G        3G                                            galium aparine  3G     3G        0                                             Russian thistle 0      0         0                                             shepherd's purse                                                                               8G     6G        4G                                            kochia          0      0         0                                             black nightshade                                                                               0      0         0                                             speedwell       0      0         0                                             wild buckwheat  0      0         0                                             sugar beet      0      0         0                                             ______________________________________                                                       Compound 3                                                                     Preemergence                                                     Rate kg/ha      0.125  0.064     0.032                                                                               0.016                                    ______________________________________                                         wheat           0      0         0    0                                        barley          0      0         0    0                                        wild oats       0      0         0    0                                        cheatgrass      5G     0         0    0                                        blackgrass      9G     9G        6G   5G                                       annual bluegrass                                                                               0      0         0    0                                        green foxtail   0      0         0    0                                        Italian ryegrass                                                                               0      0         0    0                                        rapeseed        9G     6G        2G   0                                        Matricaria inodora                                                                             7G     7G        5G   4G                                       galium aparine  5G     5G        3G   0                                        Russian thistle 0      0         0    0                                        shepherd's purse                                                                               9G     8G        8G   8G                                       kochia          10C    5G        0    0                                        black nightshade                                                                               6G     3G        2G   0                                        speedwell       10C    8G        7G   0                                        wild buckwheat  7G     0         0    0                                        sugar beet      8G     7G        2G   4G                                       ______________________________________                                                       Preemergence                                                     Rate kg/ha      0.008  0.004     0.002                                         ______________________________________                                         wheat           0      0         0                                             barley          0      0         0                                             wild oats       0      0         0                                             cheatgrass      0      0         0                                             blackgrass      5G     4G        2G                                            annual bluegrass                                                                               0      0         0                                             green foxtail   0      0         0                                             Italian ryegrass                                                                               0      0         0                                             rapeseed        0      0         0                                             Matricaria inodora                                                                             2G     0         0                                             galium aparine  0      0         0                                             Russian thistle 0      0         0                                             shepherd's purse                                                                               8G     7G        4G                                            kochia          0      0         0                                             black nightshade                                                                               0      0         0                                             speedwell       0      0         0                                             wild buckwheat  0      0         0                                             sugar beet      2G     0         0                                             ______________________________________                                                       Compound 5                                                                     Postemergence                                                    Rate kg/ha      0.125  0.064     0.032                                                                               0.016                                    ______________________________________                                         wheat           1G     0         0    0                                        barley          2G     0         0    0                                        wild oats       0      0         0    0                                        cheatgrass      5G     2G        2G   0                                        blackgrass      8G     8G        7G   6G                                       annual bluegrass                                                                               4G     3G        2G   0                                        green foxtail   0      0         0    0                                        Italian ryegrass                                                                               2G     0         0    0                                        rapeseed        10C    10C       10C  10C                                      Matricaria inodora                                                                             10C    10C       10C  10C                                      galium aparine  10C    10C       10C  10C                                      Russian thistle 10C    10C       10C  10C                                      shepherd's purse                                                                               10C    10C       9G,7C                                                                               9G,7C                                    kochia          10C    10C       10C  8G                                       black nightshade                                                                               10C    10C       9G,7C                                                                               9G,7C                                    speedwell       10C    10C       10C  10C                                      wild buckwheat  10C    10C       0    0                                        sugar beet      10C    10C       10C  10C                                      ______________________________________                                                       Postemergence                                                    Rate kg/ha      0.008  0.004     0.002                                                                               0.001                                    wheat           0      0         0    0                                        barley          0      0         0    0                                        wild oats       0      0         0    0                                        cheatgrass      0      0         0    0                                        blackgrass      2G     0         0    0                                        annual bluegrass                                                                               0      0         0    0                                        green foxtail   0      0         0    0                                        Italian ryegrass                                                                               0      0         0    0                                        rapeseed        10C    10C       10C  10C                                      Matricaria inodora                                                                             10C    10C       7G   6G                                       galium aparine  10C    7G        4G   4G                                       Russian thistle 10C    9G        9G   8G                                       shepherd's purse                                                                               10C    9G,5C     7G   7G                                       kochia          8G     8G        6G   5G                                       black nightshade                                                                               9G,7C  9G,5C     7G   6G                                       speedwell       10C    9G        6G   6G                                       wild buckwheat  0      0         0    0                                        sugar beet      10C    10C       9G   8G                                       ______________________________________                                                       Compound 5                                                                     Preemergence                                                     Rate kg/ha      0.125  0.064     0.032                                                                               0.016                                    ______________________________________                                         wheat           0      0         0    0                                        barley          0      0         0    0                                        wild oats       0      0         0    0                                        cheatgrass      5G     4G        4G   3G                                       blackgrass      6G     6G        6G   4G                                       annual bluegrass                                                                               4G     4G        3G   0                                        green foxtail   0      0         0    0                                        Italian ryegrass                                                                               4G     2G        2G   0                                        rapeseed        9G     6G        3G   3G                                       Matricaria inodora                                                                             9G     8G        8G   8G                                       galium aparine  7G     7G        7G   7G                                       Russian thistle 4G     3G        0    0                                        shepherd's purse                                                                               9G     8G        8G   7G                                       kochia          7G     5G        0    0                                        black nightshade                                                                               9G,5G  8G        4G   3G                                       speedwell       8G     8G        7G   5G                                       wild buckwheat  4G     3G        0    0                                        sugar beet      7G     6G        5G   5G                                       ______________________________________                                                       Preemergence                                                     Rate kg/ha      0.008  0.004     0.002                                                                               0.001                                    ______________________________________                                         wheat           0      0         0    0                                        barley          0      0         0    0                                        wild oats       0      0         0    0                                        cheatgrass      1G     0         0    0                                        blackgrass      4G     2G        0    0                                        annual bluegrass                                                                               0      0         0    0                                        green foxtail   0      0         0    0                                        Italian ryegrass                                                                               0      0         0    0                                        rapeseed        3G     3G        3G   3G                                       Matricaria inodora                                                                             7G     7G        0    0                                        galium aparine  6G     0         0    0                                        Russian thistle 0      0         0    0                                        shepherd's purse                                                                               3G     0         0    0                                        kochia          0      0         0    0                                        black nightshade                                                                               0      0         0    0                                        speedwell       0      0         0    0                                        wild buckwheat  0      0         0    0                                        sugar beet      4G     2G        0    0                                        ______________________________________                                     

What is claimed is:
 1. A compound of the structural formula ##STR38## wherein R is H or CH₃ ;R₁ is C₁ -C₃ alkyl, C₃ -C₄ alkoxyalkyl, C₂ -C₄ haloalkyl, C₃ -C₄ alkenyl or C₃ -C₄ alkynyl; R₂ is C₁ -C₃ alkyl, cyclopropyl, C₁ -C₃ alkylthio, C₁ -C₃ alkylsulfinyl, C₁ -C₃ alkylsulfonyl, allyloxy, allylthio, allylsulfinyl, allylsulfonyl, propargyloxy, propargylthio, propargylsulfinyl, propargylsulfonyl, OCF₂ H, C₂ -C₃ haloalkoxy, C₁ -C₃ alkyl substituted with 1-3 atoms of F or Cl, C₁ -C₂ alkyl substituted with C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio, C₁ -C₂ alkylsulfinyl, C₁ -C₂ haloalkylsulfinyl, C₁ -C₂ alkylsulfonyl, C₁ -C₂ haloalkylsulfonyl, OH or OC(O)C₁ -C₂ alkyl, C₁ -C₂ alkoxy substituted with C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio, C₁ -C₂ alkylsulfinyl, C₁ -C₂ haloalkylsulfinyl, C₁ -C.sub. 2 alkylsulfonyl, C₁ -C₂ haloalkylsulfonyl or CN, OCH₂ CH₂ NH₂, OCH₂ CH₂ NHCH₃, OCH₂ CH₂ N(CH₃)₂, C₁ -C₂ alkylthio substituted by C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio or CN, SCF₂ H, C₂ -C₃ haloalkylthio, C₁ -C₃ haloalkylsulfinyl, C₁ -C₃ haloalkylsulfonyl, C₂ -C₃ alkenyl, NR_(b) R_(c) or OC(O)C₁ -C₂ alkyl; R_(b) is H or C₁ -C₂ alkyl; R_(c) is C₁ -C₂ alkyl or C₁ -C₂ haloalkyl; Y is, OCH₃ andtheir agriculturally suitable salts.
 2. The compounds of claim 1 whereinR₂ is C₁ -C₃ alkyl, cyclopropyl, C₁ -C₃ alkylthio, C₁ -C₃ alkylsulfinyl, C₁ -C₃ alkylsulfonyl, allyloxy, allylthio, allylsulfinyl, allylsulfonyl, propargyloxy, propargylthio, propargylsulfinyl, propargylsulfonyl, OCF₂ H, OCH₂ CH₂ F, OCH₂ CHF₂, OCH₂ CF₃, OCH₂ CH₂ Cl or C₁ -C₃ alkyl substituted with 1-3 atoms of F or Cl, C₁ -C₂ alkyl substituted with OCH₃ or SCH₃.
 3. The compounds of claim 2 whereinR₂ is C₁ -C₂ alkyl, C₁ -C₂ alkoxy, C₁ -C₃ alkylthio, C₁ -C₃ alkylsulfinyl, C₁ -C₃ alkylsulfonyl, CF₃, propargyloxy, propargylthio, propargylsulfinyl, propargylsulfonyl, OCF₂ H, OCH₂ CH₂ F, OCH₂ CHF₂, OCH₂ CF₃, OCH₂ CH₂ Cl, CH₂ CH₂ OCH₃ or CH₂ CH₂ SCH₃.
 4. The compounds of claim 3 whereinR is H; R₁ is C₁ -C₂ alkyl; R₂ is C₁ -C₂ alkyl, C₁ -C₂ alkylthio, CF₃ or OCF₂ H; and Y is CH₃ or OCH₃.
 5. The compounds of claim 4 whereinR₂ is CH₃, OCH₂ CH₃ or CF₃.
 6. The compounds of claim 1 whereinR₂ is n-propyl, isopropyl, cyclopropyl, allylthio, allylsulfinyl, allylsulfonyl, C₂ -C₃ alkenyl, OC(O)CH₃, OC(O)CH₂ CH₃, CH₂ F, CHF₂, C₂ -C₃ alkyl substituted with 1-3 atoms of F, C₁ -C₃ alkyl substituted with 1-3 atoms of Cl, CH₂ OH, CH(CH₃)OH, CH₂ OCH₃, CH₂ OCH₂ CH₃, CH₂ (CH₃)OCH₃, CH₂ (CH₃)OCH₂ CH₃, CH₂ SCH₃, CH₂ SCH₂ CH₃, CH₂ (CH₃)SCH₃, CH₂ (CH₃)SCH₂ CH₃, CH₂ OC(O)C₁ -C₂ alkyl, CH(CH₃)OC(O)C₁ -C₂ alkyl, CH₂ OC₁ -C₂ haloalkyl of at least 3 halogens, CH₂ SC₁ -C₂ haloalkyl of at least 3 halogens, CH₂ S(O)C₁ -C₂ haloalkyl of at least 3 halogens, CH₂ SO₂ C₁ -C₂ haloalkyl of at least 3 halogens, CH(CH₃)OC₁ -C₂ haloalkyl of at least 3 halogens, CH(CH₃)SC₁ -C₂ haloalkyl of at least 3 halogens, CH(CH₃)S(O)C₁ -C₂ haloalkyl of at least 3 halogens, CH(CH₃)SO₂ C₁ -C₂ haloalkyl of at least 3 halogens, CH₂ CH₂ S(O)C₁ -C₂ haloalkyl or CH₂ CH₂ SO₂ C₁ -C₂ haloalkyl.
 7. The compounds of claim 6 whereinR₂ is propyl, isopropyl, cyclopropyl, allylthio, allylsulfinyl, allylsulfonyl, CH₂ OCH₃, CH(CH₃)OCH₃, CH₂ SCH₃, CH(CH₃)SCH₃, CH₂ F, CHF₂, C₂ -C₃ alkyl substituted with 1-3 atoms of F or C₁ -C₃ alkyl substituted with 1-3 atoms of Cl.
 8. The compounds of claim 1 whereinR₂ is C₁ -C₃ alkyl, SCH₃, SO₂ CH₃, CF₃ or NR_(b) R_(c).
 9. The compounds of claim 1 whereinR₂ is C₁ -C₂ alkoxy substituted with CN, OCH₂ C H₂ NH₂, OCH₂ CH₂ N(CH₃) or C₁ -C₂ alkylthio substituted by CN.
 10. The compounds of claim 9 whereinR₂ is OCH₂ CH₂ CN, OCH₂ CH₂ NH₂, OCH₂ CH₂ N(CH₃) or SCH₂ CH₂ CN.
 11. The compounds of claim 1 whereinR₂ is CH₂ CH₂ OC₁ -C₂ alkyl, CH₂ CH₂ SC₁ -C₂ alkyl, CH₂ CH₂ S(O)C₁ -C₂ alkyl, CH₂ CH₂ SO₂ C₁ -C₂ alkyl, CH₂ CH₂ OC₁ -C₂ haloalkyl, CH₂ CH₂ CH₂ SC₁ -C₂ haloalkyl, CH₂ OC₁ -C₂ haloalkyl of 1 or 2 halogens, CHHd 2SC₁ -C₂ haloalkyl of 1 or 2 halogens, CH₂ S(O)C₁ -C₂ haloalkyl of 1 or 2 halogens, CH₂ SO₂ C₁ -C₂ haloalkyl of 1 or 2 halogens, CH(CH₂)OC₁ -C₂ haloalkyl of 1 or 2 halogens, CH(CH₃)SC₁ -C₂ haloalkyl of 1 or 2 halogens, CH(CH₃)S(O)C₁ -C₂ haloalkyl of 1 or 2 halogens, or CH(CH₃)SO₂ C₁ -C₂ haloalkyl of 1 or 2 halogens.
 12. The compounds of claim 1 whereinR₂ is propargyloxy, propargylsulfinyl or propargylsulfonyl.
 13. The compounds of claim 1 whereinR₂ is allyloxy, allylthio, allylsulfinyl, allylsulfonyl, OCF₂ H, C₂ -C₃ haloalkoxy, C₁ -C₂ alkoxy substituted with C₁ -C₂ alkoxy, C₁ -C₂ haloalkyl, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio, C₁ -C₂ alkylsulfinyl, C₁ -C₂ haloalkylsulfinyl, C₁ -C₂ alkylsulfonyl or C₁ -C₂ haloalkylsulfonyl, SCF₂ H, C₂ -C₃ haloalkylthio, C₁ -C₃ haloalkylsulfinyl or C₁ -C₃ haloalkylsulfonyl.
 14. The compounds of claim 13 whereinR₂ is allyloxy, allylthio, allylsulfinyl, allylsulfonyl, OCF₂ H, OCH₂ CF₃, OCH₂ CH₂ OCH₃, OCH₂ CH₂ OCH₂ CH₃, OCH₂ CH₂ OCH₂ CF₃, OCH₂ CH₂ OCF₂ H, OCH₂ CH₂ SCH₃, OCH₂ CH₂ SCH₂ CF₃, OCH₂ CH₂ S(O)CH₃, OCH₂ CH₂ S(O)CH₂ CF₃, OCH₂ CH₂ SO₂ CH₃, OCH₂ CH₂ SO₂ CH₂ CF₃, SCF₂ H, SCH₂ CF₃, S(O)CH₂ CF₃ or SO₂ CH₂ CF₃.
 15. The compounds of claim 1 whereinR₂ is OCF₂ H, C₂ -C₃ haloalkoxy, C₁ -C₂ alkoxy substituted with C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio, C₁ -C₂ haloalkylthio, C₁ -C₂ alkylsulfinyl, C₁ -C₂ haloalkylsulfinyl, C₁ -C₂ alkylsulfonyl or C₁ -C₂ haloalkylsulfonyl, C₁ -C₂ alkylthio substituted by C₁ -C₂ alkoxy, C₁ -C₂ haloalkoxy, C₁ -C₂ alkylthio or C₁ -C₂ haloalkylthio, SCF₂ H, C₂ -C₃ haloalkylthio, C₁ -C₃ haloalkylsulfinyl or C₁ -C₃ haloalkylsulfonyl.
 16. The compounds of claim 15 whereinR₂ is OCF₂ H, OCH₂ CF₃, OCH₂ CH₂ OCH₃, OCH₂ CH₂ OCH₂ CH₃, OCH₂ CH₂ OCH₂ CF₃, OCH₂ CH₂ OCF₂ H, OCH₂ CH₂ SCH₃, OCH₂ CH₂ SCH₂ CF₃, OCH₂ CH₂ S(O)CH₃, OCH₂ CH₂ S(O)CH₂ CF₃, OCH₂ CH₂ SO₂ CH₃, OCH₂ CH₂ SO₂ CH₂ CF₃, SCH₂ CH₂ OCH₃, SCH₂ CH₂ OCH₂ CH₃, SCH₂ CH₂ OCH₂ CF₃, SCH₂ CH₂ SCH₃, SCH₂ CH₂ SCH₂ CF₃, SCF₂ H, SCH₂ CF₃, S(O)CH₂ CF₃ or SO₂ CH₂ CF₃.
 17. The compounds of claim 1 whereinR₂ is C₁ -C₃ alkyl substituted with 1-3 atoms of F or Cl.
 18. The compounds of claim 17 whereinR₂ is CF₃, CF₂ H, CFH₂, CCL₂ H or CH₂ Cl.
 19. The compounds of claim 1 whereinR₂ is C₁ -C₂ alkyl, C₁ -C₃ alkylthio, C₁ -C₃ alkylsulfinyl, C₁ -C₃ alkylsulfonyl, CF₃ or NR_(b) R_(c).
 20. The compounds of claim 19 whereinR₂ is CH₃, CH₂ CH₃, OCH₃, OCH₂ CH₃, SCH₃, SCH₂ CH₃, SCH(CH₃)₂, S(O)CH₃, S(O)CH₂ CH₃, S(O)CH(CH₃)₂, SO₂ CH₃, SO₂ CH₂ CH₃, SO₂ CH(CH₃)₂, CF₃, NHCH₃ or N(CH₃)₂.
 21. The compound of claim 1 that is 2-[[[4-(difluoromethoxy)-6-methoxypyrimidin-2-yl]aminocarbonyl]aminosulfonyl]-4-ethoxybenzoic acid, methyl ester.
 22. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 1 and at least one of the following: surfactant, solid or liquid diluent.
 23. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 2 and at least one of the following: surfactant, solid or liquid diluent.
 24. An agriculturally suitable composition for controlling the growth of undesirable vegetation comprising an effective amount of a compound of claim 3 and at least one of the following: surfactant, solid or liquid diluent.
 25. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 4 and at least one of the following: surfactant, solid or liquid diluent.
 26. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 5 and at least one of the following: surfactant, solid or liquid diluent.
 27. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 6 and at least one of the following: surfactant, solid or liquid diluent.
 28. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 8 and at least one of the following: surfactant, solid or liquid diluent.
 29. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 9 and at least one of the following: surfactant, solid or liquid diluent.
 30. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 11 and at least one of the following: surfactant, solid or liquid diluent.
 31. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 12 and at least one of the following: surfactant, solid or liquid diluent.
 32. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 13 and at least one of the following: surfactant, solid or liquid diluent.
 33. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 15 and at least one of the following: surfactant, solid or liquid diluent.
 34. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 17 and at least one of the following: surfactant, solid or liquid diluent.
 35. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 19 and at least one of the following: surfactant, solid or liquid diluent.
 36. An agriculturally suitable composition for controlling the growth of undesired vegetation comprising an effective amount of a compound of claim 21 and at least one of the following: surfactant, solid or liquid diluent.
 37. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 1. 38. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 2. 39. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 3. 40. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 4. 41. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 5. 42. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 6. 43. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 8. 44. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 9. 45. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 11. 46. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 12. 47. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 13. 48. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 15. 49. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 17. 50. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 19. 51. A method for controlling the growth of undesired vegetation which comprises applying to the locus of the crop to be protected an effective amount of a compound of claim
 21. 